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id="ProfileCheckPaperUpdate-react-component-146a139e-2742-45b3-ae47-934ec69f9770"></div> <div class="DesignSystem"><div class="onsite-ping" id="onsite-ping"></div></div><div class="profile-user-info DesignSystem"><div class="social-profile-container"><div class="left-panel-container"><div class="user-info-component-wrapper"><div class="user-summary-cta-container"><div class="user-summary-container"><div class="social-profile-avatar-container"><img class="profile-avatar u-positionAbsolute" border="0" alt="" src="//a.academia-assets.com/images/s200_no_pic.png" /></div><div class="title-container"><h1 class="ds2-5-heading-sans-serif-sm">Michael Kassiou</h1><div class="affiliations-container fake-truncate js-profile-affiliations"><div><a class="u-tcGrayDarker" href="https://sydney.academia.edu/">The University of Sydney</a>, <a class="u-tcGrayDarker" href="https://sydney.academia.edu/Departments/School_of_Chemistry/Documents">School of Chemistry</a>, <span class="u-tcGrayDarker">Faculty 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href="https://www.academia.edu/7365469/Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands"><img alt="Research paper thumbnail of Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands" class="work-thumbnail" src="https://attachments.academia-assets.com/33962609/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/7365469/Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands">Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://csu-au.academia.edu/fadyakladios">fady akladios</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="019e24b7fa720970c6f02773dd22e0a6" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":33962609,"asset_id":7365469,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/33962609/download_file?st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper 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window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='7365469']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span><span><script>$(function() { new Works.PaperRankView({ workId: 7365469, container: "", }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-f77ea15d77ce96025a6048a514272ad8becbad23c641fc2b3bd6e24ca6ff1932.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (true){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "019e24b7fa720970c6f02773dd22e0a6" } } $('.js-work-strip[data-work-id=7365469]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":7365469,"title":"Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands","translated_title":"","metadata":{"grobid_abstract":"In our continued exploration of disubstituted piperazine derivatives as sigma (r) receptor ligands with central nervous system (CNS) activity, a series of N-(2-benzofuranylmethyl)-N 0 -(methoxyphenylalkyl)piperazines (16-21 and 26-31) were synthesized, anticipating that these ligands would better suit the structural requirements of the current r 1 pharmacophore. Affinities of these ligands for r 1 and r 2 receptors were investigated by means of radioligand binding assays, with the identification of N-(2-benzofuranylmethyl)-N 0 -[3-(4-methoxyphenyl)propyl]piperazine (29, K i = 3.1 nM, r 2 /r 1 = 45) as a selective r 1 ligand. The r 1 affinities and subtype selectivities of piperazines 16-21 and 26-31 were generally comparable to the corresponding benzylic analogs. Additionally, the affinities of 16-21 and 26-31 for the 5-HT 2B receptor were much lower than the relatively nonselective methoxybenzylic analogs 2-4, indicating that elongation of the alkyl tether generally improved selectivity for r 1 receptors.","grobid_abstract_attachment_id":33962609},"translated_abstract":null,"internal_url":"https://www.academia.edu/7365469/Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands","translated_internal_url":"","created_at":"2014-06-16T09:55:15.733-07:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":8088176,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":26265190,"work_id":7365469,"tagging_user_id":8088176,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands"},{"id":26265191,"work_id":7365469,"tagging_user_id":8088176,"tagged_user_id":null,"co_author_invite_id":3708130,"email":"s***2@stanford.edu","display_order":4194304,"name":"Samuel Banister","title":"Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands"}],"downloadable_attachments":[{"id":33962609,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/33962609/thumbnails/1.jpg","file_name":"akladios2.pdf","download_url":"https://www.academia.edu/attachments/33962609/download_file?st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Effects_of_linker_elongation_in_a_series.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/33962609/akladios2-libre.pdf?1402937710=\u0026response-content-disposition=attachment%3B+filename%3DEffects_of_linker_elongation_in_a_series.pdf\u0026Expires=1732999528\u0026Signature=UJDdCNzAfhJgYgQgBN5FQtZd8Z0bfGqnPH3Le6mztCFs8YenZnQrVheZgQTBuHRT-YFLnWODLt3P3TSfj4fPFCp5cZ1oWw6EZDN0PCS8pS2N5A5C7BFSesLYBfMTSJVcCb2b15~3FsSM-qcc7aojzcFCoCFRcEb7dJ9wrUsvNjTmIx~4L943vYsr1YCZzs-mHAcJFT9sx0YNz6Gc8a1JhngS6-w1nv4Vk6BABhEcDpMT3YsPhaBND-UBR9yP6ULIvGh8yMQ~4t0Qtx4g42DFOB6N4SnkpbX6p6MpwqJG-2Amiw5FF1AYc3x9fTOf3YNezj3nIHge74fllMs92mtONQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands","translated_slug":"","page_count":4,"language":"en","content_type":"Work","owner":{"id":8088176,"first_name":"fady","middle_initials":null,"last_name":"akladios","page_name":"fadyakladios","domain_name":"csu-au","created_at":"2014-01-07T09:13:32.895-08:00","display_name":"fady akladios","url":"https://csu-au.academia.edu/fadyakladios"},"attachments":[{"id":33962609,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/33962609/thumbnails/1.jpg","file_name":"akladios2.pdf","download_url":"https://www.academia.edu/attachments/33962609/download_file?st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Effects_of_linker_elongation_in_a_series.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/33962609/akladios2-libre.pdf?1402937710=\u0026response-content-disposition=attachment%3B+filename%3DEffects_of_linker_elongation_in_a_series.pdf\u0026Expires=1732999528\u0026Signature=UJDdCNzAfhJgYgQgBN5FQtZd8Z0bfGqnPH3Le6mztCFs8YenZnQrVheZgQTBuHRT-YFLnWODLt3P3TSfj4fPFCp5cZ1oWw6EZDN0PCS8pS2N5A5C7BFSesLYBfMTSJVcCb2b15~3FsSM-qcc7aojzcFCoCFRcEb7dJ9wrUsvNjTmIx~4L943vYsr1YCZzs-mHAcJFT9sx0YNz6Gc8a1JhngS6-w1nv4Vk6BABhEcDpMT3YsPhaBND-UBR9yP6ULIvGh8yMQ~4t0Qtx4g42DFOB6N4SnkpbX6p6MpwqJG-2Amiw5FF1AYc3x9fTOf3YNezj3nIHge74fllMs92mtONQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[{"id":635,"name":"Psychiatry","url":"https://www.academia.edu/Documents/in/Psychiatry"}],"urls":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="27100356"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/27100356/The_pharmacology_of_valinate_and_tert_leucinate_synthetic_cannabinoids_5F_AMBICA_5F_AMB_5F_ADB_AMB_FUBINACA_MDMB_FUBINACA_MDMB_CHMICA_and_their_analogues"><img alt="Research paper thumbnail of The pharmacology of valinate and tert-leucinate synthetic cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and their analogues" class="work-thumbnail" src="https://attachments.academia-assets.com/47351890/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/27100356/The_pharmacology_of_valinate_and_tert_leucinate_synthetic_cannabinoids_5F_AMBICA_5F_AMB_5F_ADB_AMB_FUBINACA_MDMB_FUBINACA_MDMB_CHMICA_and_their_analogues">The pharmacology of valinate and tert-leucinate synthetic cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and their analogues</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Indole and indazole synthetic cannabinoids (SCs) featuring L-valinate or L-tert-leucinate pendant...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Indole and indazole synthetic cannabinoids (SCs) featuring L-valinate or L-tert-leucinate pendant group have recently emerged as prevalent recreational drugs, and their use has been associated with serious adverse health effects. Due to the limited pharmacological data available for these compounds, 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA and their analogues were synthesized and assessed for cannabimimetic activity in vitro and in vivo. All SCs acted as potent, highly efficacious agonists at CB1 (EC50 = 0.45–36 nM) and CB2 (EC50 = 4.6–128 nM) receptors in a fluorometric assay of membrane potential, with a general preference for CB1 activation. The cannabimimetic properties of two prevalent compounds with confirmed toxicity in humans, 5F-AMB and MDMB-FUBINACA, were demonstrated in vivo using biotelemetry in rats. Bradycardia and hypothermia were induced by 5F-AMB and MDMB-FUBINACA doses of 0.1–1 mg/kg (and 3 mg/kg for 5F-AMB), with MDMB-FUBINACA showing the most dramatic hypothermic response recorded in our laboratory for any SC (>3 ºC at 0.3 mg/kg). Reversal of hypothermia by pretreatment with a CB1, but not CB2, antagonist was demonstrated for 5F-AMB and MDMB-FUBINACA, consistent with CB1-mediated effects in vivo.  The in vitro and in vivo data indicate that these SCs act as highly efficacious CB receptor agonists with greater potency than ∆9-THC and earlier generations of SCs.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d026559fdb8b43aba2350ac855127de7" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":47351890,"asset_id":27100356,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/47351890/download_file?st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="27100356"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="27100356"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 27100356; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=27100356]").text(description); $(".js-view-count[data-work-id=27100356]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 27100356; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='27100356']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span><span><script>$(function() { new Works.PaperRankView({ workId: 27100356, container: "", }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-f77ea15d77ce96025a6048a514272ad8becbad23c641fc2b3bd6e24ca6ff1932.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (true){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "d026559fdb8b43aba2350ac855127de7" } } $('.js-work-strip[data-work-id=27100356]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":27100356,"title":"The pharmacology of valinate and tert-leucinate synthetic cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and their analogues","translated_title":"","metadata":{"abstract":"Indole and indazole synthetic cannabinoids (SCs) featuring L-valinate or L-tert-leucinate pendant group have recently emerged as prevalent recreational drugs, and their use has been associated with serious adverse health effects. Due to the limited pharmacological data available for these compounds, 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA and their analogues were synthesized and assessed for cannabimimetic activity in vitro and in vivo. All SCs acted as potent, highly efficacious agonists at CB1 (EC50 = 0.45–36 nM) and CB2 (EC50 = 4.6–128 nM) receptors in a fluorometric assay of membrane potential, with a general preference for CB1 activation. The cannabimimetic properties of two prevalent compounds with confirmed toxicity in humans, 5F-AMB and MDMB-FUBINACA, were demonstrated in vivo using biotelemetry in rats. Bradycardia and hypothermia were induced by 5F-AMB and MDMB-FUBINACA doses of 0.1–1 mg/kg (and 3 mg/kg for 5F-AMB), with MDMB-FUBINACA showing the most dramatic hypothermic response recorded in our laboratory for any SC (\u003e3 ºC at 0.3 mg/kg). Reversal of hypothermia by pretreatment with a CB1, but not CB2, antagonist was demonstrated for 5F-AMB and MDMB-FUBINACA, consistent with CB1-mediated effects in vivo. The in vitro and in vivo data indicate that these SCs act as highly efficacious CB receptor agonists with greater potency than ∆9-THC and earlier generations of SCs."},"translated_abstract":"Indole and indazole synthetic cannabinoids (SCs) featuring L-valinate or L-tert-leucinate pendant group have recently emerged as prevalent recreational drugs, and their use has been associated with serious adverse health effects. Due to the limited pharmacological data available for these compounds, 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA and their analogues were synthesized and assessed for cannabimimetic activity in vitro and in vivo. All SCs acted as potent, highly efficacious agonists at CB1 (EC50 = 0.45–36 nM) and CB2 (EC50 = 4.6–128 nM) receptors in a fluorometric assay of membrane potential, with a general preference for CB1 activation. The cannabimimetic properties of two prevalent compounds with confirmed toxicity in humans, 5F-AMB and MDMB-FUBINACA, were demonstrated in vivo using biotelemetry in rats. Bradycardia and hypothermia were induced by 5F-AMB and MDMB-FUBINACA doses of 0.1–1 mg/kg (and 3 mg/kg for 5F-AMB), with MDMB-FUBINACA showing the most dramatic hypothermic response recorded in our laboratory for any SC (\u003e3 ºC at 0.3 mg/kg). Reversal of hypothermia by pretreatment with a CB1, but not CB2, antagonist was demonstrated for 5F-AMB and MDMB-FUBINACA, consistent with CB1-mediated effects in vivo. 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="26384121"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/26384121/The_recent_development_of_%CE%B17_nicotinic_acetylcholine_receptor_nAChR_ligands_as_therapeutic_candidates_for_the_treatment_of_central_nervous_system_CNS_diseases"><img alt="Research paper thumbnail of The recent development of α7 nicotinic acetylcholine receptor (nAChR) ligands as therapeutic candidates for the treatment of central nervous system (CNS) diseases" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/26384121/The_recent_development_of_%CE%B17_nicotinic_acetylcholine_receptor_nAChR_ligands_as_therapeutic_candidates_for_the_treatment_of_central_nervous_system_CNS_diseases">The recent development of α7 nicotinic acetylcholine receptor (nAChR) ligands as therapeutic candidates for the treatment of central nervous system (CNS) diseases</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d6952135b6429b40ed1ca7b0cc3a4a05" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":46686259,"asset_id":26384121,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/46686259/download_file?st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="26384121"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="26384121"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 26384121; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="22608419"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/22608419/Trishomocubanes_Novel_%CF%83_ligands_modulate_cocaine_induced_behavioural_effects"><img alt="Research paper thumbnail of Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects" class="work-thumbnail" src="https://attachments.academia-assets.com/43207870/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/22608419/Trishomocubanes_Novel_%CF%83_ligands_modulate_cocaine_induced_behavioural_effects">Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="32faadf4ddf6e4319b9113de88122325" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":43207870,"asset_id":22608419,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/43207870/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="22608419"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="22608419"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 22608419; 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TC1 and TC4 have high affinity and moderate to high selectivity for σ 1 (Ki = 10 nM, σ 1 /σ 2 = 0.03) and σ 2 (Ki = 20 nM, σ 1 /σ 2 = 7.6) receptor subtypes respectively. Both compounds have negligible affinity for the dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters. In behavioural studies, TC1 produced a dose-related inhibition in spontaneous locomotor activity measured in a Digiscan apparatus. TC1 attenuated the stimulatory locomotor effect of 20 mg/kg cocaine with a half-maximal depressant activity (ID 50 ) of 38.6 mg/kg. TC1 (dose range of 25 to 100 mg/kg) also partially substituted for the effect of cocaine (10 mg/kg) in a discriminative stimulus task, involving the trained discrimination between cocaine and saline using a two-lever choice method. Following a dose of 50 mg/kg TC1, a maximum of 31% substitution was reached. The response rate was reduced to 56% of vehicle control following a TC1 dose of 100 mg/kg. These behavioural effects suggest that TC1 can act as an antagonist via the σ 1 receptor. In contrast to TC1, TC4 produced a stimulant effect in locomotor activity with the ED 50 estimated at 0.94 mg/kg. In addition, TC4 failed to inhibit cocaine-induced stimulation; neither did it substitute for the discriminative stimulus effects of cocaine. TC4 thus appears to interact predominantly with the σ 2 receptor subtype (σ 1 /σ 2 = 7.6) which may result in dopamine stimulation independent of the effects of cocaine. The differential effect of TC1 and TC4 warrants further study of the mechanism of these actions. Present data also suggests a potential role for trishomocubane analogues in developing medication or research tools for cocaine addiction.","publication_date":{"day":18,"month":10,"year":2006,"errors":{}},"grobid_abstract_attachment_id":43207870},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608419/Trishomocubanes_Novel_%CF%83_ligands_modulate_cocaine_induced_behavioural_effects","translated_internal_url":"","created_at":"2016-02-29T10:07:51.943-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":18772976,"work_id":22608419,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects"},{"id":18942049,"work_id":22608419,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":1813629,"email":"s***e@sydney.edu.au","display_order":4194304,"name":"Steven Meikle","title":"Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects"},{"id":18942050,"work_id":22608419,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":2695564,"email":"r***i@usyd.edu.au","display_order":6291456,"name":"Richard Banati","title":"Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects"}],"downloadable_attachments":[{"id":43207870,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207870/thumbnails/1.jpg","file_name":"2007_-_EJP_-_anti-cocaine.pdf","download_url":"https://www.academia.edu/attachments/43207870/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Trishomocubanes_Novel__ligands_modulate.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207870/2007_-_EJP_-_anti-cocaine-libre.pdf?1456769253=\u0026response-content-disposition=attachment%3B+filename%3DTrishomocubanes_Novel__ligands_modulate.pdf\u0026Expires=1732999529\u0026Signature=SqSJCJYzgcue5JGFFa5JjuZq0lgJdx3Z5fZQ7iLQ5xszaTrm9Fha~rDRYuPls1cemZS0GEkZH5w4LXLNWXeyAKQP9bxogwoyrnbVc7PSBlup5bOA-6ak7zZg2SEwIf0sleVfhhdCPKD2Y1JYqmVAZilPvxlv55tX-eKttK9wh0Us761D~Wv-~evST7DzhudrXXWOipocE5ExbWrZEkgwRrVeVo0B13xtAWlanlw7j8cuUwJp0okxvfmfEl8eKPogu~tSHWf7wVuDiJVuMYAtqLgYRl4Cu3x0pGwhdbdbxZFtStqe38ZBCkY41kyjBLAWSliAMafMpULlCswlehpaQQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Trishomocubanes_Novel_σ_ligands_modulate_cocaine_induced_behavioural_effects","translated_slug":"","page_count":6,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207870,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207870/thumbnails/1.jpg","file_name":"2007_-_EJP_-_anti-cocaine.pdf","download_url":"https://www.academia.edu/attachments/43207870/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Trishomocubanes_Novel__ligands_modulate.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207870/2007_-_EJP_-_anti-cocaine-libre.pdf?1456769253=\u0026response-content-disposition=attachment%3B+filename%3DTrishomocubanes_Novel__ligands_modulate.pdf\u0026Expires=1732999529\u0026Signature=SqSJCJYzgcue5JGFFa5JjuZq0lgJdx3Z5fZQ7iLQ5xszaTrm9Fha~rDRYuPls1cemZS0GEkZH5w4LXLNWXeyAKQP9bxogwoyrnbVc7PSBlup5bOA-6ak7zZg2SEwIf0sleVfhhdCPKD2Y1JYqmVAZilPvxlv55tX-eKttK9wh0Us761D~Wv-~evST7DzhudrXXWOipocE5ExbWrZEkgwRrVeVo0B13xtAWlanlw7j8cuUwJp0okxvfmfEl8eKPogu~tSHWf7wVuDiJVuMYAtqLgYRl4Cu3x0pGwhdbdbxZFtStqe38ZBCkY41kyjBLAWSliAMafMpULlCswlehpaQQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854437,"url":"http://dx.doi.org/10.1016/j.ejphar.2006.10.020"}]}, dispatcherData: dispatcherData }); 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Examination of in vitro σ 1 {[ 3 H](þ)-pentazocine} and σ 2 ([ 3 H]DTG) receptor binding profiles of piperazines 11-13 and 25-36 revealed several highly potent and σ 1 selective ligands, notably, N-(benzofuran-2-ylmethyl)-N 0 -(4 0 -methoxybenzyl)piperazine (13, K i = 2.7 nM, σ 2 /σ 1 = 38) and N-(benzofuran-2-ylmethyl)-N 0 -(4 0 -(2 00 -fluoroethoxy)benzyl)piperazine (30, K i = 2.6 nM, σ 2 /σ 1 = 187). Structural features for optimal σ 1 receptor affinity and selectivity over the σ 2 receptor were identified. On the basis of its favorable log D value, 13 was selected as a candidate for the development of a σ 1 receptor positron emission tomography radiotracer. [ 11 C]13 showed high uptake in the brain and other σ receptor-rich organs of a Papio hamadryas baboon. 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This letter details a concise synthetic sequence that gives ready access to DBH on gram scale. The route features a Staudinger reduction of an azide to facilitate a transannular cyclisation Ó 2013 Elsevier Ltd. All rights reserved.","publication_date":{"day":27,"month":7,"year":2013,"errors":{}},"grobid_abstract_attachment_id":43207900},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608449/A_practical_synthesis_of_1S_4S_2_5_diazabicyclo_2_2_1_heptane","translated_internal_url":"","created_at":"2016-02-29T10:07:52.160-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577171,"work_id":22608449,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane"},{"id":16577172,"work_id":22608449,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":3720148,"email":"c***t@stanford.edu","display_order":4194304,"name":"Corinne Beinat","title":"A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane"},{"id":16577173,"work_id":22608449,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":2344845,"email":"c***n@sydney.edu.au","display_order":6291456,"name":"Christopher McErlean","title":"A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane"}],"downloadable_attachments":[{"id":43207900,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207900/thumbnails/1.jpg","file_name":"2013_-_TetLett_-_DBH.pdf","download_url":"https://www.academia.edu/attachments/43207900/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"A_practical_synthesis_of_1S_4S_2_5_diaza.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207900/2013_-_TetLett_-_DBH-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3DA_practical_synthesis_of_1S_4S_2_5_diaza.pdf\u0026Expires=1732999529\u0026Signature=UvmKONqk~xta7NxkYOFauHfsiQuxvq7MG~KSQwXd31lAdhT3MY9jJyl1jmHQzI6mnPZ879UmfyYK~WbykD7wuxqZw1NzgImrHg0hDs9hR~~iWbM2o0GhclSN8ensSMB4l0uzvnxOLroHK-VuXSOgHWuiWcVgqBht~MRNUxD~fnzPk4Hhzlg3y4CR9Bh5fIT~~U6IScnDQZcSknHZbZL4UIi4-vjpGWbOduItKpBF~eDgZtSRYLG7jSvYanAzcFxhnkhqYPCr3TrLahBQX3M55OxSVgTD1WWmUE2g~D8MoxPMoE0wS~dI-c0cbs1Q1r7ctBtEG22JqetlxnO0wyerHA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"A_practical_synthesis_of_1S_4S_2_5_diazabicyclo_2_2_1_heptane","translated_slug":"","page_count":3,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207900,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207900/thumbnails/1.jpg","file_name":"2013_-_TetLett_-_DBH.pdf","download_url":"https://www.academia.edu/attachments/43207900/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"A_practical_synthesis_of_1S_4S_2_5_diaza.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207900/2013_-_TetLett_-_DBH-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3DA_practical_synthesis_of_1S_4S_2_5_diaza.pdf\u0026Expires=1732999529\u0026Signature=UvmKONqk~xta7NxkYOFauHfsiQuxvq7MG~KSQwXd31lAdhT3MY9jJyl1jmHQzI6mnPZ879UmfyYK~WbykD7wuxqZw1NzgImrHg0hDs9hR~~iWbM2o0GhclSN8ensSMB4l0uzvnxOLroHK-VuXSOgHWuiWcVgqBht~MRNUxD~fnzPk4Hhzlg3y4CR9Bh5fIT~~U6IScnDQZcSknHZbZL4UIi4-vjpGWbOduItKpBF~eDgZtSRYLG7jSvYanAzcFxhnkhqYPCr3TrLahBQX3M55OxSVgTD1WWmUE2g~D8MoxPMoE0wS~dI-c0cbs1Q1r7ctBtEG22JqetlxnO0wyerHA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854281,"url":"http://dx.doi.org/10.1016/j.tetlet.2013.07.092"}]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="22608447"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/22608447/Structure_activity_relationships_of_synthetic_cannabinoid_designer_drug_RCS_4_and_its_regioisomers_and_C4_homologues"><img alt="Research paper thumbnail of Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues" class="work-thumbnail" src="https://attachments.academia-assets.com/43207896/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/22608447/Structure_activity_relationships_of_synthetic_cannabinoid_designer_drug_RCS_4_and_its_regioisomers_and_C4_homologues">Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="2fc13f87107f0c05768a9435146a5cfe" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":43207896,"asset_id":22608447,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/43207896/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="22608447"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="22608447"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 22608447; 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dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "2fc13f87107f0c05768a9435146a5cfe" } } $('.js-work-strip[data-work-id=22608447]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":22608447,"title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues","translated_title":"","metadata":{"journal_name":"Forensic Toxicology","grobid_abstract":"-1-yl-(1-pentyl-1Hindol-3-yl)methanone] represents the first of several Nalkyl-3-(methoxybenzoyl)indoles identified by forensic scientists as synthetic cannabinoid (SC) designer drugs. Despite the detection of RCS-4 and several analogues (RCS-2, RCS-3, RCS-2-C4, RCS-3-C4, and RCS-4-C4) in products intended for human consumption, relatively little is known about this class of cannabinoids. The synthesis of all regioisomers of RCS-4 and their C4 homologues is described. This study also systematically explored the structure-activity relationships of this class of SCs at human CB 1 and CB 2 receptors using an in vitro fluorometric imaging plate reader membrane potential assay. All compounds demonstrated agonist activity at CB 1 (EC 50 = 54-574 nM) and CB 2 (EC 50 = 4.5-46 nM) receptors, with the C4 homologues showing a preference for CB 2 receptors over CB 1 receptors (31-42 times). Since most of the analogues (RCS-2, RCS-3, RCS-2-C4, RCS-3-C4 and RCS-4-C4) are not subject to regulation in much of the world, despite their activities towards CB 1 and CB 2 receptors, there is a possibility that these analogues will emerge on the black market. 0.26) to give 10 as a colorless oil (2.90 g, 84 %). 1 H NMR (500 MHz, CDCl 3 ): d 7.70 (1H, d, J = 8.0 Hz), 7.41 (1H, d, J = 8.0 Hz), 7.27 (1H, dd, J = 8.8, 8.0 Hz), 7.12-7.09 (2H, m), 6.55 (1H, d, J = 4.0 Hz), 4.16 (2H, t, J = 7.2 Hz), 1.86 (2H, quin., J = 7.6 Hz), 1.41 (2H, quin., J = 7.6 Hz), 1.0 (3H, t, J = 7.6 Hz). All spectroscopic data matched those previously reported .","publication_date":{"day":31,"month":5,"year":2015,"errors":{}},"grobid_abstract_attachment_id":43207896},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608447/Structure_activity_relationships_of_synthetic_cannabinoid_designer_drug_RCS_4_and_its_regioisomers_and_C4_homologues","translated_internal_url":"","created_at":"2016-02-29T10:07:52.178-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577174,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 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href="https://www.academia.edu/22608448/Ether_analogues_of_DPA_714_with_subnanomolar_affinity_for_the_translocator_protein_TSPO_">Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a>, <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a>, and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SSelleri">S. 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All analogues showed superior binding affinities for TSPO compared to DPA-713 (5) and DPA-714 (6). Picomolar affinities were observed for this class of TSPO ligands in this assay for the first time, with phenethyl ether 28 showing the greatest affinity (K i ¼ 0.13 nM). Additionally, all analogues increased pregnenolone biosynthesis (134e331% above baseline) in a rat C6 glioma cell steroidogenesis assay.","publication_date":{"day":7,"month":2,"year":2015,"errors":{}},"grobid_abstract_attachment_id":43207901},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608448/Ether_analogues_of_DPA_714_with_subnanomolar_affinity_for_the_translocator_protein_TSPO_","translated_internal_url":"","created_at":"2016-02-29T10:07:52.178-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577184,"work_id":22608448,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)"},{"id":16577185,"work_id":22608448,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":601542,"email":"c***i@unipi.it","display_order":4194304,"name":"Claudia Martini","title":"Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)"},{"id":16577186,"work_id":22608448,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":3720148,"email":"c***t@stanford.edu","display_order":6291456,"name":"Corinne Beinat","title":"Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)"},{"id":16577187,"work_id":22608448,"tagging_user_id":44167404,"tagged_user_id":44064025,"co_author_invite_id":null,"email":"s***n@sydney.edu.au","display_order":7340032,"name":"Shane Wilkinson","title":"Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)"},{"id":16577188,"work_id":22608448,"tagging_user_id":44167404,"tagged_user_id":39141499,"co_author_invite_id":null,"email":"d***o@farm.unipi.it","affiliation":"University of Pisa","display_order":7864320,"name":"Eleonora Da Pozzo","title":"Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)"},{"id":21599562,"work_id":22608448,"tagging_user_id":44167404,"tagged_user_id":31070696,"co_author_invite_id":null,"email":"s***i@unifi.it","display_order":8126464,"name":"S. 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The historical development of selective s 1 receptor ligands as potential PET imaging agents, as well as the radiochemistry and application of the most recently developed examples, is described herein.","publication_date":{"day":24,"month":4,"year":2013,"errors":{}},"grobid_abstract_attachment_id":43207890},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608429/The_development_of_radiotracers_for_imaging_sigma_%CF%83_receptors_in_the_central_nervous_system_CNS_using_positron_emission_tomography_PET_","translated_internal_url":"","created_at":"2016-02-29T10:07:52.059-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577314,"work_id":22608429,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"The development of radiotracers for imaging sigma (σ) receptors in the central nervous system (CNS) using positron emission tomography (PET)"}],"downloadable_attachments":[{"id":43207890,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207890/thumbnails/1.jpg","file_name":"2013_-_JLCR_-_Sigma_radiochem.pdf","download_url":"https://www.academia.edu/attachments/43207890/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"The_development_of_radiotracers_for_imag.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207890/2013_-_JLCR_-_Sigma_radiochem-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DThe_development_of_radiotracers_for_imag.pdf\u0026Expires=1732999529\u0026Signature=YaFK~FlnxhFq0WQ3UPIGo1kffsx8gBV3JjcvopIUvKdVuIOPXukrl1nzkLwSGM613Sd7KLalNnfb6WtT3X4irQbJb6~K6~5Xr~LrcAbWXScAxP6yZ3T4pi73Zp7uIMIE~7a2IDuNFIdH3C5dbnKdlVFUM~M~CKB1J21JHa7TOkd~XpANBcnAOqhr8rdF6Ka-8cSzdr4YyAdAfElpde3x-pjjRZD4GhNDcH2Ey7E3UAiHcsjxnjrOSekuSiGk2HuOC3IREOUcuveBdrEy9tdVVmN5gj8lT7SYGWMbroQ7UTu6fmGZ4NFDq5Yv1f2cb~d0zq-FfTGoZ78ENO6VQ-6vAA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"The_development_of_radiotracers_for_imaging_sigma_σ_receptors_in_the_central_nervous_system_CNS_using_positron_emission_tomography_PET_","translated_slug":"","page_count":10,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207890,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207890/thumbnails/1.jpg","file_name":"2013_-_JLCR_-_Sigma_radiochem.pdf","download_url":"https://www.academia.edu/attachments/43207890/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"The_development_of_radiotracers_for_imag.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207890/2013_-_JLCR_-_Sigma_radiochem-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DThe_development_of_radiotracers_for_imag.pdf\u0026Expires=1732999529\u0026Signature=YaFK~FlnxhFq0WQ3UPIGo1kffsx8gBV3JjcvopIUvKdVuIOPXukrl1nzkLwSGM613Sd7KLalNnfb6WtT3X4irQbJb6~K6~5Xr~LrcAbWXScAxP6yZ3T4pi73Zp7uIMIE~7a2IDuNFIdH3C5dbnKdlVFUM~M~CKB1J21JHa7TOkd~XpANBcnAOqhr8rdF6Ka-8cSzdr4YyAdAfElpde3x-pjjRZD4GhNDcH2Ey7E3UAiHcsjxnjrOSekuSiGk2HuOC3IREOUcuveBdrEy9tdVVmN5gj8lT7SYGWMbroQ7UTu6fmGZ4NFDq5Yv1f2cb~d0zq-FfTGoZ78ENO6VQ-6vAA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854290,"url":"http://dx.doi.org/10.1002/jlcr.3010"}]}, dispatcherData: dispatcherData }); 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window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=22608426]").text(description); $(".js-view-count[data-work-id=22608426]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 22608426; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='22608426']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span><span><script>$(function() { new Works.PaperRankView({ workId: 22608426, container: "", }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-f77ea15d77ce96025a6048a514272ad8becbad23c641fc2b3bd6e24ca6ff1932.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (true){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "89c35919296db84958c26d30af76902d" } } $('.js-work-strip[data-work-id=22608426]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":22608426,"title":"N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (σ) receptor ligands","translated_title":"","metadata":{"journal_name":"Bioorganic \u0026 Medicinal Chemistry Letters","grobid_abstract":"A series of racemic N-arylalkyl-2-azaadamantan-1-ols (9-15) and the corresponding deoxygenated, achiral N-arylalkyl-2-azaadamantanes (23-29) were synthesized and screened in competition binding assays against a panel of CNS targets. Adamantyl hemiaminals 9-15 displayed generally low affinity for both r 1 (K i values = 294-1950 nM) and r 2 receptors (K i values = 201-1020 nM), and negligible affinity for 42 other CNS proteins. Deoxygenation of 9-15 to give the corresponding achiral azaadamantanes 23-29 greatly improved affinity for r 1 (K i values = 8.3-239 nM) and r 2 receptors (K i values = 34-312 nM).","publication_date":{"day":14,"month":7,"year":2011,"errors":{}},"grobid_abstract_attachment_id":43207880},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608426/N_Arylalkyl_2_azaadamantanes_as_cage_expanded_polycarbocyclic_sigma_%CF%83_receptor_ligands","translated_internal_url":"","created_at":"2016-02-29T10:07:52.045-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577315,"work_id":22608426,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (σ) receptor ligands"}],"downloadable_attachments":[{"id":43207880,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207880/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Aza-adamantanes.pdf","download_url":"https://www.academia.edu/attachments/43207880/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"N_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207880/2011_-_BMCL_-_Aza-adamantanes-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DN_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf\u0026Expires=1732999529\u0026Signature=SMEGHavnmuSmA78r5Op6NSGnwKKIZXd6~lrzUIndDplEG8pABb1eIhUeQ9y2bORO1FfFXIhhYl1fqJJt~w~TLlaptUqfVKX~sGo-dGQS6NRlyHS7xmRZ-LLZKiKTlakVpziT7sd7awZU6xa30wqcygSG6Eck0-NGEDBChObFRdN7PTb2f8FJXPYkRiWNWrJMdnKIpt72g9UjuA-Q7r7SU5JpmdWL2z6qewQFrmzcUAJW6XK9GPVVtGrB~wz8qdlCQK3HVrYOZKJr6D9HlJgRjX5G0SzfAowuKNYyrkkL8iHgHVkYi3lq0unH0oqUYRp7zpi3JImjyLo46IDManPmPw__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"N_Arylalkyl_2_azaadamantanes_as_cage_expanded_polycarbocyclic_sigma_σ_receptor_ligands","translated_slug":"","page_count":4,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207880,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207880/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Aza-adamantanes.pdf","download_url":"https://www.academia.edu/attachments/43207880/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"N_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207880/2011_-_BMCL_-_Aza-adamantanes-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DN_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf\u0026Expires=1732999529\u0026Signature=SMEGHavnmuSmA78r5Op6NSGnwKKIZXd6~lrzUIndDplEG8pABb1eIhUeQ9y2bORO1FfFXIhhYl1fqJJt~w~TLlaptUqfVKX~sGo-dGQS6NRlyHS7xmRZ-LLZKiKTlakVpziT7sd7awZU6xa30wqcygSG6Eck0-NGEDBChObFRdN7PTb2f8FJXPYkRiWNWrJMdnKIpt72g9UjuA-Q7r7SU5JpmdWL2z6qewQFrmzcUAJW6XK9GPVVtGrB~wz8qdlCQK3HVrYOZKJr6D9HlJgRjX5G0SzfAowuKNYyrkkL8iHgHVkYi3lq0unH0oqUYRp7zpi3JImjyLo46IDManPmPw__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854410,"url":"http://dx/doi.org/10.1016/j.bmcl.2011.07.028"}]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="22608430"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/22608430/Synthesis_and_in_vivo_evaluation_of_18F_N_2_benzofuranylmethyl_N_4_2_fluoroethoxy_benzyl_piperazine_a_novel_%CF%831_receptor_PET_imaging_agent"><img alt="Research paper thumbnail of Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent" class="work-thumbnail" src="https://attachments.academia-assets.com/43207887/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/22608430/Synthesis_and_in_vivo_evaluation_of_18F_N_2_benzofuranylmethyl_N_4_2_fluoroethoxy_benzyl_piperazine_a_novel_%CF%831_receptor_PET_imaging_agent">Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="bb890a3485f5d4ec2fdc8a310abf7f30" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":43207887,"asset_id":22608430,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/43207887/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="22608430"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="22608430"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 22608430; 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Radiofluorination of the appropriate tosylate precursor furnished [ 18 F]6 with a specific activity of 45 GBq/lmol, in an average radiochemical yield of 18% and greater than 98% radiochemical purity. Micro-PET imaging in Papio hamadryas baboon brain revealed [ 18 F]6 uptake consistent with r receptor distribution, and specificity for r receptors was demonstrated in a haloperidol pre-treated animal. 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Agents such as the clinical oncology tracer 2-[ 18 F]fluoro-2-deoxy-Dglucose ([ 18 F]FDG), the most widely used PET-radiopharmaceutical, are driving an increasing interest in the chemistry of radiopharmaceuticals utilizing fluorine-18. This review outlines the methods for production of fluorine-18, and the development of agents for performing radiofluorination reactions. With a few exceptions, radiofluorinations can be classified as either electrophilic or nucleophilic. The electrophilic reactions mainly use molecular [ 18 F]fluorine of moderately low specific radioactivity, or reagents prepared from it, and include additions to alkenes, reactions with carbanions and especially fluorodehydrogenation and fluorodemetallation. The nucleophilic reactions usually involve no-carrier-added (highspecific-radioactivity) [ 18 F]fluoride as its K[ 18 F]F-K 222 complex and include S N 2-type substitutions in the aliphatic series and S N Ar-type substitutions in the aromatic and heteroaromatic series. Key examples from each class of radiofluorination reaction will be described, highlighting the potential of this radioisotope in the design and preparation of fluorine-18labeled probes for PET imaging.","publication_date":{"day":null,"month":null,"year":2010,"errors":{}},"grobid_abstract_attachment_id":43207874},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608433/Fluorine_18_Chemistry_for_PET_A_Concise_Introduction","translated_internal_url":"","created_at":"2016-02-29T10:07:52.066-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577294,"work_id":22608433,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Fluorine-18 Chemistry for PET: A Concise Introduction"},{"id":16577295,"work_id":22608433,"tagging_user_id":44167404,"tagged_user_id":48835427,"co_author_invite_id":429660,"email":"f***e@cea.fr","display_order":4194304,"name":"Frédéric Dollé","title":"Fluorine-18 Chemistry for PET: A Concise Introduction"}],"downloadable_attachments":[{"id":43207874,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207874/thumbnails/1.jpg","file_name":"2010_-_CurrRadiopharm_-_F18_for_PET_intro_review.pdf","download_url":"https://www.academia.edu/attachments/43207874/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Fluorine_18_Chemistry_for_PET_A_Concise.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207874/2010_-_CurrRadiopharm_-_F18_for_PET_intro_review-libre.pdf?1456769258=\u0026response-content-disposition=attachment%3B+filename%3DFluorine_18_Chemistry_for_PET_A_Concise.pdf\u0026Expires=1732999529\u0026Signature=dlm1mqDYRok1wJrhsWIeMgyYpijeLQQvZv10FbeSqI3KzKCPbnxkU6PgWS7RNVRYiY3oP25uZfNbv-CPOuNng6j9uzg1bCINkCRt3RhVH6yeIpl~te3yWJ5E86jmb91YxFIWFW7VDJZmWFUzIojdWHeS5RjzAl5Ej7agLsa8mNj6d2bdBYoAfzZN4yPg-nkLEpdew8nzrunMEqNFqqwS-hhuPUXcmKsCwmdkj3I86bByWUIrddUBiJrcDZsZwGE~8FoERXjsgWBlhePCsyXqIxRNcK3IMEP-HiMBova0grViJYWe-tnd2vx3Gf1M57gkTJkkKxfOQCO11PISDxToaA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Fluorine_18_Chemistry_for_PET_A_Concise_Introduction","translated_slug":"","page_count":13,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207874,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207874/thumbnails/1.jpg","file_name":"2010_-_CurrRadiopharm_-_F18_for_PET_intro_review.pdf","download_url":"https://www.academia.edu/attachments/43207874/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Fluorine_18_Chemistry_for_PET_A_Concise.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207874/2010_-_CurrRadiopharm_-_F18_for_PET_intro_review-libre.pdf?1456769258=\u0026response-content-disposition=attachment%3B+filename%3DFluorine_18_Chemistry_for_PET_A_Concise.pdf\u0026Expires=1732999529\u0026Signature=dlm1mqDYRok1wJrhsWIeMgyYpijeLQQvZv10FbeSqI3KzKCPbnxkU6PgWS7RNVRYiY3oP25uZfNbv-CPOuNng6j9uzg1bCINkCRt3RhVH6yeIpl~te3yWJ5E86jmb91YxFIWFW7VDJZmWFUzIojdWHeS5RjzAl5Ej7agLsa8mNj6d2bdBYoAfzZN4yPg-nkLEpdew8nzrunMEqNFqqwS-hhuPUXcmKsCwmdkj3I86bByWUIrddUBiJrcDZsZwGE~8FoERXjsgWBlhePCsyXqIxRNcK3IMEP-HiMBova0grViJYWe-tnd2vx3Gf1M57gkTJkkKxfOQCO11PISDxToaA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854424,"url":"http://dx.doi.org/10.2174/1874471011003020068"}]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="22608431"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/22608431/Insights_into_Structure_Activity_Relationships_and_CNS_Therapeutic_Applications_of_NR2B_Selective_Antagonists"><img alt="Research paper thumbnail of Insights into Structure-Activity Relationships and CNS Therapeutic Applications of NR2B Selective Antagonists" class="work-thumbnail" src="https://attachments.academia-assets.com/43207883/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/22608431/Insights_into_Structure_Activity_Relationships_and_CNS_Therapeutic_Applications_of_NR2B_Selective_Antagonists">Insights into Structure-Activity Relationships and CNS Therapeutic Applications of NR2B Selective Antagonists</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="550fc2c1a200513c4a7ac200e4a35303" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":43207883,"asset_id":22608431,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/43207883/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="22608431"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="22608431"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 22608431; 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The use of NMDA antagonists as therapeutic agents has been restricted as a result of unwanted side effects including hallucinations and loss of co-ordination. NR2B subtype selective antagonists have previously shown a therapeutic effect without causing the side effects of broad spectrum NMDA antagonists. Considerable research has since been devoted to the development of orally bioavailable, selective NR2B antagonists and their applications in various neurological diseases. The improved therapeutic index of these compounds is expected to be the result of the subtype selectivity and cellular location of the NR2B receptors within the CNS. 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Affinities of these ligands for r 1 and r 2 receptors were investigated by means of radioligand binding assays, with the identification of N-(2-benzofuranylmethyl)-N 0 -[3-(4-methoxyphenyl)propyl]piperazine (29, K i = 3.1 nM, r 2 /r 1 = 45) as a selective r 1 ligand. The r 1 affinities and subtype selectivities of piperazines 16-21 and 26-31 were generally comparable to the corresponding benzylic analogs. Additionally, the affinities of 16-21 and 26-31 for the 5-HT 2B receptor were much lower than the relatively nonselective methoxybenzylic analogs 2-4, indicating that elongation of the alkyl tether generally improved selectivity for r 1 receptors.","publication_date":{"day":12,"month":8,"year":2011,"errors":{}},"grobid_abstract_attachment_id":43207875},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608432/Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_methoxyphenylalkyl_piperazine_%CF%831_receptor_ligands","translated_internal_url":"","created_at":"2016-02-29T10:07:52.064-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577296,"work_id":22608432,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazine σ1 receptor ligands"}],"downloadable_attachments":[{"id":43207875,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207875/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Piperazines_elongation.pdf","download_url":"https://www.academia.edu/attachments/43207875/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Effects_of_linker_elongation_in_a_series.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207875/2011_-_BMCL_-_Piperazines_elongation-libre.pdf?1456769253=\u0026response-content-disposition=attachment%3B+filename%3DEffects_of_linker_elongation_in_a_series.pdf\u0026Expires=1732999529\u0026Signature=Q8sfKljfg8-xISw2FHPdPb4UtRckiTz8g9UmSn5FvyBoWQE9rCD1L2zvbqcXYsepqYYF0Doc~nTHZ1FZW7B-5tJ-YbT5Pr8X3OVFxRhu9r1HgIZFrjyDVBG8nFxh9vt-QRhyKPnn4EDHdr5ClekTNM2tduE1YraDnQfw9re2T-a3U0diHRM9aSR~XsFfTphtpcj0~UCwf5XKq4gd-aGE506dHs4~W29WSa3iKbDHFO0dzTt~ZGhpVWqi3kFz~a7fZzP-KzxbC5Zfucp3ek-bNIVwDVuG0TsQ1o4LaKrJqOlg6h8P7tQ0F5blRNNUEUJZMqwyx7qKv0bogAesM-MPEQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_methoxyphenylalkyl_piperazine_σ1_receptor_ligands","translated_slug":"","page_count":4,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207875,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207875/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Piperazines_elongation.pdf","download_url":"https://www.academia.edu/attachments/43207875/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Effects_of_linker_elongation_in_a_series.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207875/2011_-_BMCL_-_Piperazines_elongation-libre.pdf?1456769253=\u0026response-content-disposition=attachment%3B+filename%3DEffects_of_linker_elongation_in_a_series.pdf\u0026Expires=1732999529\u0026Signature=Q8sfKljfg8-xISw2FHPdPb4UtRckiTz8g9UmSn5FvyBoWQE9rCD1L2zvbqcXYsepqYYF0Doc~nTHZ1FZW7B-5tJ-YbT5Pr8X3OVFxRhu9r1HgIZFrjyDVBG8nFxh9vt-QRhyKPnn4EDHdr5ClekTNM2tduE1YraDnQfw9re2T-a3U0diHRM9aSR~XsFfTphtpcj0~UCwf5XKq4gd-aGE506dHs4~W29WSa3iKbDHFO0dzTt~ZGhpVWqi3kFz~a7fZzP-KzxbC5Zfucp3ek-bNIVwDVuG0TsQ1o4LaKrJqOlg6h8P7tQ0F5blRNNUEUJZMqwyx7qKv0bogAesM-MPEQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854391,"url":"http://dx.doi.org/10.1016/j.bmcl.2011.08.029"}]}, dispatcherData: dispatcherData }); 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In vitro competition binding assays against r receptors revealed that arylalkyl N-substituents conferred selectivity for the r 2 subtype, while alicyclic or polycarbocyclic substituents imparted high affinity for both subtypes. The r 2 binding and subtype selectivities of N-arylalkyl-7-azanorbornanes was generally greater than the analogously-substituted pyrrolidines, indicating that steric bulk and conformational restriction around the nitrogen atom are likely important for subtype discrimination.","publication_date":{"day":30,"month":4,"year":2012,"errors":{}},"grobid_abstract_attachment_id":43207891},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608437/7_Azabicyclo_2_2_1_heptane_as_a_scaffold_for_the_development_of_selective_sigma_2_%CF%832_receptor_ligands","translated_internal_url":"","created_at":"2016-02-29T10:07:52.105-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577288,"work_id":22608437,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (σ2) receptor ligands"},{"id":16577289,"work_id":22608437,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":1371353,"email":"l***a@sydney.edu.au","display_order":4194304,"name":"Louis Rendina","title":"7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (σ2) receptor ligands"}],"downloadable_attachments":[{"id":43207891,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207891/thumbnails/1.jpg","file_name":"2012_-_BMCL_-_Azabicycloheptanes.pdf","download_url":"https://www.academia.edu/attachments/43207891/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"7_Azabicyclo_2_2_1_heptane_as_a_scaffold.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207891/2012_-_BMCL_-_Azabicycloheptanes-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3D7_Azabicyclo_2_2_1_heptane_as_a_scaffold.pdf\u0026Expires=1732999529\u0026Signature=RToaRPAx0b8fk7DHV6IxwDooHx~dIGn3VNUHyiBFmiSrJ6HQwp3Nbp43geRpwUNnDpLP~ApVMDUJAYKzFCxq1rE0EVnqWOk8Mo7Y3O3bKlMb8Is0Yl75UUFtfUW-dGpS7tpbD9unNnTBvmi72HcfSuGCeUUPfs1P~23RPA~4bozBuIXnFzJvz7x5ti05cU-iKwmi7BB6KP8-VDdvFZluE3qnExvqSF1V4dWRCNh0bVo8IQ031RjvJTxCiTLk73NIee-KM~AZxb6dOY6uHDBanpcmp~94-3TY9dGpJvrVxBtfO1MnIaWKf-bgMnu0tbsqZBe4vh0zJXVNf8jbksMicA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"7_Azabicyclo_2_2_1_heptane_as_a_scaffold_for_the_development_of_selective_sigma_2_σ2_receptor_ligands","translated_slug":"","page_count":5,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207891,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207891/thumbnails/1.jpg","file_name":"2012_-_BMCL_-_Azabicycloheptanes.pdf","download_url":"https://www.academia.edu/attachments/43207891/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"7_Azabicyclo_2_2_1_heptane_as_a_scaffold.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207891/2012_-_BMCL_-_Azabicycloheptanes-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3D7_Azabicyclo_2_2_1_heptane_as_a_scaffold.pdf\u0026Expires=1732999529\u0026Signature=RToaRPAx0b8fk7DHV6IxwDooHx~dIGn3VNUHyiBFmiSrJ6HQwp3Nbp43geRpwUNnDpLP~ApVMDUJAYKzFCxq1rE0EVnqWOk8Mo7Y3O3bKlMb8Is0Yl75UUFtfUW-dGpS7tpbD9unNnTBvmi72HcfSuGCeUUPfs1P~23RPA~4bozBuIXnFzJvz7x5ti05cU-iKwmi7BB6KP8-VDdvFZluE3qnExvqSF1V4dWRCNh0bVo8IQ031RjvJTxCiTLk73NIee-KM~AZxb6dOY6uHDBanpcmp~94-3TY9dGpJvrVxBtfO1MnIaWKf-bgMnu0tbsqZBe4vh0zJXVNf8jbksMicA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854366,"url":"http://dx.doi.org/10.1016/j.bmcl.2012.04.077"}]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> </div><div class="profile--tab_content_container js-tab-pane tab-pane" data-section-id="3773369" id="papers"><div class="js-work-strip profile--work_container" data-work-id="7365469"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/7365469/Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands"><img alt="Research paper thumbnail of Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands" class="work-thumbnail" src="https://attachments.academia-assets.com/33962609/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/7365469/Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands">Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://csu-au.academia.edu/fadyakladios">fady akladios</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="019e24b7fa720970c6f02773dd22e0a6" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":33962609,"asset_id":7365469,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/33962609/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="7365469"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="7365469"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 7365469; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=7365469]").text(description); $(".js-view-count[data-work-id=7365469]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 7365469; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='7365469']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span><span><script>$(function() { new Works.PaperRankView({ workId: 7365469, container: "", }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-f77ea15d77ce96025a6048a514272ad8becbad23c641fc2b3bd6e24ca6ff1932.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (true){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); 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Affinities of these ligands for r 1 and r 2 receptors were investigated by means of radioligand binding assays, with the identification of N-(2-benzofuranylmethyl)-N 0 -[3-(4-methoxyphenyl)propyl]piperazine (29, K i = 3.1 nM, r 2 /r 1 = 45) as a selective r 1 ligand. The r 1 affinities and subtype selectivities of piperazines 16-21 and 26-31 were generally comparable to the corresponding benzylic analogs. Additionally, the affinities of 16-21 and 26-31 for the 5-HT 2B receptor were much lower than the relatively nonselective methoxybenzylic analogs 2-4, indicating that elongation of the alkyl tether generally improved selectivity for r 1 receptors.","grobid_abstract_attachment_id":33962609},"translated_abstract":null,"internal_url":"https://www.academia.edu/7365469/Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands","translated_internal_url":"","created_at":"2014-06-16T09:55:15.733-07:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":8088176,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":26265190,"work_id":7365469,"tagging_user_id":8088176,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands"},{"id":26265191,"work_id":7365469,"tagging_user_id":8088176,"tagged_user_id":null,"co_author_invite_id":3708130,"email":"s***2@stanford.edu","display_order":4194304,"name":"Samuel Banister","title":"Effects of linker elongation in a series of N-(2-benzofuranylmethyl)- N 0 -(methoxyphenylalkyl)piperazine r 1 receptor ligands"}],"downloadable_attachments":[{"id":33962609,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/33962609/thumbnails/1.jpg","file_name":"akladios2.pdf","download_url":"https://www.academia.edu/attachments/33962609/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Effects_of_linker_elongation_in_a_series.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/33962609/akladios2-libre.pdf?1402937710=\u0026response-content-disposition=attachment%3B+filename%3DEffects_of_linker_elongation_in_a_series.pdf\u0026Expires=1732999528\u0026Signature=UJDdCNzAfhJgYgQgBN5FQtZd8Z0bfGqnPH3Le6mztCFs8YenZnQrVheZgQTBuHRT-YFLnWODLt3P3TSfj4fPFCp5cZ1oWw6EZDN0PCS8pS2N5A5C7BFSesLYBfMTSJVcCb2b15~3FsSM-qcc7aojzcFCoCFRcEb7dJ9wrUsvNjTmIx~4L943vYsr1YCZzs-mHAcJFT9sx0YNz6Gc8a1JhngS6-w1nv4Vk6BABhEcDpMT3YsPhaBND-UBR9yP6ULIvGh8yMQ~4t0Qtx4g42DFOB6N4SnkpbX6p6MpwqJG-2Amiw5FF1AYc3x9fTOf3YNezj3nIHge74fllMs92mtONQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Effects_of_linker_elongation_in_a_series_of_N_2_benzofuranylmethyl_N_0_methoxyphenylalkyl_piperazine_r_1_receptor_ligands","translated_slug":"","page_count":4,"language":"en","content_type":"Work","owner":{"id":8088176,"first_name":"fady","middle_initials":null,"last_name":"akladios","page_name":"fadyakladios","domain_name":"csu-au","created_at":"2014-01-07T09:13:32.895-08:00","display_name":"fady akladios","url":"https://csu-au.academia.edu/fadyakladios"},"attachments":[{"id":33962609,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/33962609/thumbnails/1.jpg","file_name":"akladios2.pdf","download_url":"https://www.academia.edu/attachments/33962609/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Effects_of_linker_elongation_in_a_series.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/33962609/akladios2-libre.pdf?1402937710=\u0026response-content-disposition=attachment%3B+filename%3DEffects_of_linker_elongation_in_a_series.pdf\u0026Expires=1732999528\u0026Signature=UJDdCNzAfhJgYgQgBN5FQtZd8Z0bfGqnPH3Le6mztCFs8YenZnQrVheZgQTBuHRT-YFLnWODLt3P3TSfj4fPFCp5cZ1oWw6EZDN0PCS8pS2N5A5C7BFSesLYBfMTSJVcCb2b15~3FsSM-qcc7aojzcFCoCFRcEb7dJ9wrUsvNjTmIx~4L943vYsr1YCZzs-mHAcJFT9sx0YNz6Gc8a1JhngS6-w1nv4Vk6BABhEcDpMT3YsPhaBND-UBR9yP6ULIvGh8yMQ~4t0Qtx4g42DFOB6N4SnkpbX6p6MpwqJG-2Amiw5FF1AYc3x9fTOf3YNezj3nIHge74fllMs92mtONQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[{"id":635,"name":"Psychiatry","url":"https://www.academia.edu/Documents/in/Psychiatry"}],"urls":[]}, dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="27100356"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/27100356/The_pharmacology_of_valinate_and_tert_leucinate_synthetic_cannabinoids_5F_AMBICA_5F_AMB_5F_ADB_AMB_FUBINACA_MDMB_FUBINACA_MDMB_CHMICA_and_their_analogues"><img alt="Research paper thumbnail of The pharmacology of valinate and tert-leucinate synthetic cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and their analogues" class="work-thumbnail" src="https://attachments.academia-assets.com/47351890/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/27100356/The_pharmacology_of_valinate_and_tert_leucinate_synthetic_cannabinoids_5F_AMBICA_5F_AMB_5F_ADB_AMB_FUBINACA_MDMB_FUBINACA_MDMB_CHMICA_and_their_analogues">The pharmacology of valinate and tert-leucinate synthetic cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and their analogues</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item"><span class="js-work-more-abstract-truncated">Indole and indazole synthetic cannabinoids (SCs) featuring L-valinate or L-tert-leucinate pendant...</span><a class="js-work-more-abstract" data-broccoli-component="work_strip.more_abstract" data-click-track="profile-work-strip-more-abstract" href="javascript:;"><span> more </span><span><i class="fa fa-caret-down"></i></span></a><span class="js-work-more-abstract-untruncated hidden">Indole and indazole synthetic cannabinoids (SCs) featuring L-valinate or L-tert-leucinate pendant group have recently emerged as prevalent recreational drugs, and their use has been associated with serious adverse health effects. Due to the limited pharmacological data available for these compounds, 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA and their analogues were synthesized and assessed for cannabimimetic activity in vitro and in vivo. All SCs acted as potent, highly efficacious agonists at CB1 (EC50 = 0.45–36 nM) and CB2 (EC50 = 4.6–128 nM) receptors in a fluorometric assay of membrane potential, with a general preference for CB1 activation. The cannabimimetic properties of two prevalent compounds with confirmed toxicity in humans, 5F-AMB and MDMB-FUBINACA, were demonstrated in vivo using biotelemetry in rats. Bradycardia and hypothermia were induced by 5F-AMB and MDMB-FUBINACA doses of 0.1–1 mg/kg (and 3 mg/kg for 5F-AMB), with MDMB-FUBINACA showing the most dramatic hypothermic response recorded in our laboratory for any SC (>3 ºC at 0.3 mg/kg). Reversal of hypothermia by pretreatment with a CB1, but not CB2, antagonist was demonstrated for 5F-AMB and MDMB-FUBINACA, consistent with CB1-mediated effects in vivo.  The in vitro and in vivo data indicate that these SCs act as highly efficacious CB receptor agonists with greater potency than ∆9-THC and earlier generations of SCs.</span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d026559fdb8b43aba2350ac855127de7" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":47351890,"asset_id":27100356,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/47351890/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="27100356"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="27100356"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 27100356; window.Academia.workViewCountsFetcher.queue(workId, function (count) { var description = window.$h.commaizeInt(count) + " " + window.$h.pluralize(count, 'View'); $(".js-view-count[data-work-id=27100356]").text(description); $(".js-view-count[data-work-id=27100356]").attr('title', description).tooltip(); }); });</script></span></span><span><span class="percentile-widget hidden"><span class="u-mr2x work-percentile"></span></span><script>$(function () { var workId = 27100356; window.Academia.workPercentilesFetcher.queue(workId, function (percentileText) { var container = $(".js-work-strip[data-work-id='27100356']"); container.find('.work-percentile').text(percentileText.charAt(0).toUpperCase() + percentileText.slice(1)); container.find('.percentile-widget').show(); container.find('.percentile-widget').removeClass('hidden'); }); });</script></span><span><script>$(function() { new Works.PaperRankView({ workId: 27100356, container: "", }); });</script></span></div><div id="work-strip-premium-row-container"></div></div></div><script> require.config({ waitSeconds: 90 })(["https://a.academia-assets.com/assets/wow_profile-f77ea15d77ce96025a6048a514272ad8becbad23c641fc2b3bd6e24ca6ff1932.js","https://a.academia-assets.com/assets/work_edit-ad038b8c047c1a8d4fa01b402d530ff93c45fee2137a149a4a5398bc8ad67560.js"], function() { // from javascript_helper.rb var dispatcherData = {} if (true){ window.WowProfile.dispatcher = window.WowProfile.dispatcher || _.clone(Backbone.Events); dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "d026559fdb8b43aba2350ac855127de7" } } $('.js-work-strip[data-work-id=27100356]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":27100356,"title":"The pharmacology of valinate and tert-leucinate synthetic cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and their analogues","translated_title":"","metadata":{"abstract":"Indole and indazole synthetic cannabinoids (SCs) featuring L-valinate or L-tert-leucinate pendant group have recently emerged as prevalent recreational drugs, and their use has been associated with serious adverse health effects. 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="26384121"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/26384121/The_recent_development_of_%CE%B17_nicotinic_acetylcholine_receptor_nAChR_ligands_as_therapeutic_candidates_for_the_treatment_of_central_nervous_system_CNS_diseases"><img alt="Research paper thumbnail of The recent development of α7 nicotinic acetylcholine receptor (nAChR) ligands as therapeutic candidates for the treatment of central nervous system (CNS) diseases" class="work-thumbnail" src="https://a.academia-assets.com/images/blank-paper.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/26384121/The_recent_development_of_%CE%B17_nicotinic_acetylcholine_receptor_nAChR_ligands_as_therapeutic_candidates_for_the_treatment_of_central_nervous_system_CNS_diseases">The recent development of α7 nicotinic acetylcholine receptor (nAChR) ligands as therapeutic candidates for the treatment of central nervous system (CNS) diseases</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="d6952135b6429b40ed1ca7b0cc3a4a05" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":46686259,"asset_id":26384121,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/46686259/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOCw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="26384121"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="26384121"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 26384121; 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$(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="22608419"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/22608419/Trishomocubanes_Novel_%CF%83_ligands_modulate_cocaine_induced_behavioural_effects"><img alt="Research paper thumbnail of Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects" class="work-thumbnail" src="https://attachments.academia-assets.com/43207870/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/22608419/Trishomocubanes_Novel_%CF%83_ligands_modulate_cocaine_induced_behavioural_effects">Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a> and <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a></span></div><div class="wp-workCard_item wp-workCard--actions"><span class="work-strip-bookmark-button-container"></span><a id="32faadf4ddf6e4319b9113de88122325" class="wp-workCard--action" rel="nofollow" data-click-track="profile-work-strip-download" data-download="{"attachment_id":43207870,"asset_id":22608419,"asset_type":"Work","button_location":"profile"}" href="https://www.academia.edu/attachments/43207870/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&s=profile"><span><i class="fa fa-arrow-down"></i></span><span>Download</span></a><span class="wp-workCard--action visible-if-viewed-by-owner inline-block" style="display: none;"><span class="js-profile-work-strip-edit-button-wrapper profile-work-strip-edit-button-wrapper" data-work-id="22608419"><a class="js-profile-work-strip-edit-button" tabindex="0"><span><i class="fa fa-pencil"></i></span><span>Edit</span></a></span></span><span id="work-strip-rankings-button-container"></span></div><div class="wp-workCard_item wp-workCard--stats"><span><span><span class="js-view-count view-count u-mr2x" data-work-id="22608419"><i class="fa fa-spinner fa-spin"></i></span><script>$(function () { var workId = 22608419; 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TC1 and TC4 have high affinity and moderate to high selectivity for σ 1 (Ki = 10 nM, σ 1 /σ 2 = 0.03) and σ 2 (Ki = 20 nM, σ 1 /σ 2 = 7.6) receptor subtypes respectively. Both compounds have negligible affinity for the dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters. In behavioural studies, TC1 produced a dose-related inhibition in spontaneous locomotor activity measured in a Digiscan apparatus. TC1 attenuated the stimulatory locomotor effect of 20 mg/kg cocaine with a half-maximal depressant activity (ID 50 ) of 38.6 mg/kg. TC1 (dose range of 25 to 100 mg/kg) also partially substituted for the effect of cocaine (10 mg/kg) in a discriminative stimulus task, involving the trained discrimination between cocaine and saline using a two-lever choice method. Following a dose of 50 mg/kg TC1, a maximum of 31% substitution was reached. The response rate was reduced to 56% of vehicle control following a TC1 dose of 100 mg/kg. These behavioural effects suggest that TC1 can act as an antagonist via the σ 1 receptor. In contrast to TC1, TC4 produced a stimulant effect in locomotor activity with the ED 50 estimated at 0.94 mg/kg. In addition, TC4 failed to inhibit cocaine-induced stimulation; neither did it substitute for the discriminative stimulus effects of cocaine. TC4 thus appears to interact predominantly with the σ 2 receptor subtype (σ 1 /σ 2 = 7.6) which may result in dopamine stimulation independent of the effects of cocaine. The differential effect of TC1 and TC4 warrants further study of the mechanism of these actions. Present data also suggests a potential role for trishomocubane analogues in developing medication or research tools for cocaine addiction.","publication_date":{"day":18,"month":10,"year":2006,"errors":{}},"grobid_abstract_attachment_id":43207870},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608419/Trishomocubanes_Novel_%CF%83_ligands_modulate_cocaine_induced_behavioural_effects","translated_internal_url":"","created_at":"2016-02-29T10:07:51.943-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":18772976,"work_id":22608419,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects"},{"id":18942049,"work_id":22608419,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":1813629,"email":"s***e@sydney.edu.au","display_order":4194304,"name":"Steven Meikle","title":"Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects"},{"id":18942050,"work_id":22608419,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":2695564,"email":"r***i@usyd.edu.au","display_order":6291456,"name":"Richard Banati","title":"Trishomocubanes: Novel σ ligands modulate cocaine-induced behavioural effects"}],"downloadable_attachments":[{"id":43207870,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207870/thumbnails/1.jpg","file_name":"2007_-_EJP_-_anti-cocaine.pdf","download_url":"https://www.academia.edu/attachments/43207870/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Trishomocubanes_Novel__ligands_modulate.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207870/2007_-_EJP_-_anti-cocaine-libre.pdf?1456769253=\u0026response-content-disposition=attachment%3B+filename%3DTrishomocubanes_Novel__ligands_modulate.pdf\u0026Expires=1732999529\u0026Signature=SqSJCJYzgcue5JGFFa5JjuZq0lgJdx3Z5fZQ7iLQ5xszaTrm9Fha~rDRYuPls1cemZS0GEkZH5w4LXLNWXeyAKQP9bxogwoyrnbVc7PSBlup5bOA-6ak7zZg2SEwIf0sleVfhhdCPKD2Y1JYqmVAZilPvxlv55tX-eKttK9wh0Us761D~Wv-~evST7DzhudrXXWOipocE5ExbWrZEkgwRrVeVo0B13xtAWlanlw7j8cuUwJp0okxvfmfEl8eKPogu~tSHWf7wVuDiJVuMYAtqLgYRl4Cu3x0pGwhdbdbxZFtStqe38ZBCkY41kyjBLAWSliAMafMpULlCswlehpaQQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Trishomocubanes_Novel_σ_ligands_modulate_cocaine_induced_behavioural_effects","translated_slug":"","page_count":6,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207870,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207870/thumbnails/1.jpg","file_name":"2007_-_EJP_-_anti-cocaine.pdf","download_url":"https://www.academia.edu/attachments/43207870/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Trishomocubanes_Novel__ligands_modulate.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207870/2007_-_EJP_-_anti-cocaine-libre.pdf?1456769253=\u0026response-content-disposition=attachment%3B+filename%3DTrishomocubanes_Novel__ligands_modulate.pdf\u0026Expires=1732999529\u0026Signature=SqSJCJYzgcue5JGFFa5JjuZq0lgJdx3Z5fZQ7iLQ5xszaTrm9Fha~rDRYuPls1cemZS0GEkZH5w4LXLNWXeyAKQP9bxogwoyrnbVc7PSBlup5bOA-6ak7zZg2SEwIf0sleVfhhdCPKD2Y1JYqmVAZilPvxlv55tX-eKttK9wh0Us761D~Wv-~evST7DzhudrXXWOipocE5ExbWrZEkgwRrVeVo0B13xtAWlanlw7j8cuUwJp0okxvfmfEl8eKPogu~tSHWf7wVuDiJVuMYAtqLgYRl4Cu3x0pGwhdbdbxZFtStqe38ZBCkY41kyjBLAWSliAMafMpULlCswlehpaQQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854437,"url":"http://dx.doi.org/10.1016/j.ejphar.2006.10.020"}]}, dispatcherData: dispatcherData }); 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All rights reserved.","publication_date":{"day":27,"month":7,"year":2013,"errors":{}},"grobid_abstract_attachment_id":43207900},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608449/A_practical_synthesis_of_1S_4S_2_5_diazabicyclo_2_2_1_heptane","translated_internal_url":"","created_at":"2016-02-29T10:07:52.160-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577171,"work_id":22608449,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane"},{"id":16577172,"work_id":22608449,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":3720148,"email":"c***t@stanford.edu","display_order":4194304,"name":"Corinne Beinat","title":"A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane"},{"id":16577173,"work_id":22608449,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":2344845,"email":"c***n@sydney.edu.au","display_order":6291456,"name":"Christopher McErlean","title":"A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane"}],"downloadable_attachments":[{"id":43207900,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207900/thumbnails/1.jpg","file_name":"2013_-_TetLett_-_DBH.pdf","download_url":"https://www.academia.edu/attachments/43207900/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"A_practical_synthesis_of_1S_4S_2_5_diaza.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207900/2013_-_TetLett_-_DBH-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3DA_practical_synthesis_of_1S_4S_2_5_diaza.pdf\u0026Expires=1732999529\u0026Signature=UvmKONqk~xta7NxkYOFauHfsiQuxvq7MG~KSQwXd31lAdhT3MY9jJyl1jmHQzI6mnPZ879UmfyYK~WbykD7wuxqZw1NzgImrHg0hDs9hR~~iWbM2o0GhclSN8ensSMB4l0uzvnxOLroHK-VuXSOgHWuiWcVgqBht~MRNUxD~fnzPk4Hhzlg3y4CR9Bh5fIT~~U6IScnDQZcSknHZbZL4UIi4-vjpGWbOduItKpBF~eDgZtSRYLG7jSvYanAzcFxhnkhqYPCr3TrLahBQX3M55OxSVgTD1WWmUE2g~D8MoxPMoE0wS~dI-c0cbs1Q1r7ctBtEG22JqetlxnO0wyerHA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"A_practical_synthesis_of_1S_4S_2_5_diazabicyclo_2_2_1_heptane","translated_slug":"","page_count":3,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207900,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207900/thumbnails/1.jpg","file_name":"2013_-_TetLett_-_DBH.pdf","download_url":"https://www.academia.edu/attachments/43207900/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"A_practical_synthesis_of_1S_4S_2_5_diaza.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207900/2013_-_TetLett_-_DBH-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3DA_practical_synthesis_of_1S_4S_2_5_diaza.pdf\u0026Expires=1732999529\u0026Signature=UvmKONqk~xta7NxkYOFauHfsiQuxvq7MG~KSQwXd31lAdhT3MY9jJyl1jmHQzI6mnPZ879UmfyYK~WbykD7wuxqZw1NzgImrHg0hDs9hR~~iWbM2o0GhclSN8ensSMB4l0uzvnxOLroHK-VuXSOgHWuiWcVgqBht~MRNUxD~fnzPk4Hhzlg3y4CR9Bh5fIT~~U6IScnDQZcSknHZbZL4UIi4-vjpGWbOduItKpBF~eDgZtSRYLG7jSvYanAzcFxhnkhqYPCr3TrLahBQX3M55OxSVgTD1WWmUE2g~D8MoxPMoE0wS~dI-c0cbs1Q1r7ctBtEG22JqetlxnO0wyerHA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854281,"url":"http://dx.doi.org/10.1016/j.tetlet.2013.07.092"}]}, dispatcherData: dispatcherData }); 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dispatcherData = { dispatcher: window.WowProfile.dispatcher, downloadLinkId: "2fc13f87107f0c05768a9435146a5cfe" } } $('.js-work-strip[data-work-id=22608447]').each(function() { if (!$(this).data('initialized')) { new WowProfile.WorkStripView({ el: this, workJSON: {"id":22608447,"title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues","translated_title":"","metadata":{"journal_name":"Forensic Toxicology","grobid_abstract":"-1-yl-(1-pentyl-1Hindol-3-yl)methanone] represents the first of several Nalkyl-3-(methoxybenzoyl)indoles identified by forensic scientists as synthetic cannabinoid (SC) designer drugs. Despite the detection of RCS-4 and several analogues (RCS-2, RCS-3, RCS-2-C4, RCS-3-C4, and RCS-4-C4) in products intended for human consumption, relatively little is known about this class of cannabinoids. The synthesis of all regioisomers of RCS-4 and their C4 homologues is described. This study also systematically explored the structure-activity relationships of this class of SCs at human CB 1 and CB 2 receptors using an in vitro fluorometric imaging plate reader membrane potential assay. All compounds demonstrated agonist activity at CB 1 (EC 50 = 54-574 nM) and CB 2 (EC 50 = 4.5-46 nM) receptors, with the C4 homologues showing a preference for CB 2 receptors over CB 1 receptors (31-42 times). Since most of the analogues (RCS-2, RCS-3, RCS-2-C4, RCS-3-C4 and RCS-4-C4) are not subject to regulation in much of the world, despite their activities towards CB 1 and CB 2 receptors, there is a possibility that these analogues will emerge on the black market. 0.26) to give 10 as a colorless oil (2.90 g, 84 %). 1 H NMR (500 MHz, CDCl 3 ): d 7.70 (1H, d, J = 8.0 Hz), 7.41 (1H, d, J = 8.0 Hz), 7.27 (1H, dd, J = 8.8, 8.0 Hz), 7.12-7.09 (2H, m), 6.55 (1H, d, J = 4.0 Hz), 4.16 (2H, t, J = 7.2 Hz), 1.86 (2H, quin., J = 7.6 Hz), 1.41 (2H, quin., J = 7.6 Hz), 1.0 (3H, t, J = 7.6 Hz). All spectroscopic data matched those previously reported .","publication_date":{"day":31,"month":5,"year":2015,"errors":{}},"grobid_abstract_attachment_id":43207896},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608447/Structure_activity_relationships_of_synthetic_cannabinoid_designer_drug_RCS_4_and_its_regioisomers_and_C4_homologues","translated_internal_url":"","created_at":"2016-02-29T10:07:52.178-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577174,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues"},{"id":16577175,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":308818,"email":"d***s@sydney.edu.au","display_order":4194304,"name":"David Hibbs","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues"},{"id":16577176,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":3720148,"email":"c***t@stanford.edu","display_order":6291456,"name":"Corinne Beinat","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues"},{"id":16577177,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":44064025,"co_author_invite_id":null,"email":"s***n@sydney.edu.au","display_order":7340032,"name":"Shane Wilkinson","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues"},{"id":16577178,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":3720157,"email":"j***t@mq.edu.au","display_order":7864320,"name":"Jordyn Stuart","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues"},{"id":16577181,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":88766113,"co_author_invite_id":422067,"email":"m***s@auckland.ac.nz","display_order":8126464,"name":"Myatt G","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues"},{"id":16577182,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":3800890,"email":"m***r@mq.edu.au","display_order":8257536,"name":"Mark Connor","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 homologues"},{"id":16577183,"work_id":22608447,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":230680,"email":"i***r@sydney.edu.au","display_order":8323072,"name":"Iain McGregor","title":"Structure–activity relationships of synthetic cannabinoid designer drug RCS-4 and its regioisomers and C4 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dispatcherData: dispatcherData }); $(this).data('initialized', true); } }); $a.trackClickSource(".js-work-strip-work-link", "profile_work_strip") }); </script> <div class="js-work-strip profile--work_container" data-work-id="22608448"><div class="profile--work_thumbnail hidden-xs"><a class="js-work-strip-work-link" data-click-track="profile-work-strip-thumbnail" href="https://www.academia.edu/22608448/Ether_analogues_of_DPA_714_with_subnanomolar_affinity_for_the_translocator_protein_TSPO_"><img alt="Research paper thumbnail of Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)" class="work-thumbnail" src="https://attachments.academia-assets.com/43207901/thumbnails/1.jpg" /></a></div><div class="wp-workCard wp-workCard_itemContainer"><div class="wp-workCard_item wp-workCard--title"><a class="js-work-strip-work-link text-gray-darker" data-click-track="profile-work-strip-title" href="https://www.academia.edu/22608448/Ether_analogues_of_DPA_714_with_subnanomolar_affinity_for_the_translocator_protein_TSPO_">Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)</a></div><div class="wp-workCard_item wp-workCard--coauthors"><span>by </span><span><a class="" data-click-track="profile-work-strip-authors" href="https://stanford.academia.edu/SamuelBanister">Samuel Banister</a>, <a class="" data-click-track="profile-work-strip-authors" href="https://sydney.academia.edu/MichaelKassiou">Michael Kassiou</a>, and <a class="" data-click-track="profile-work-strip-authors" href="https://independent.academia.edu/SSelleri">S. 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All analogues showed superior binding affinities for TSPO compared to DPA-713 (5) and DPA-714 (6). Picomolar affinities were observed for this class of TSPO ligands in this assay for the first time, with phenethyl ether 28 showing the greatest affinity (K i ¼ 0.13 nM). 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Excluding 3 low affinity analogs, 31 ligands demonstrated nanomolar K i values for either r receptor subtype. Several selective r 1 and r 2 ligands were discovered, with selectivities of up to 29.6 times for r 1 and 52.4 times for r 2 , as well as several high affinity, subtype non-selective ligands. The diversity of structures and r 1 affinities of the ligands allowed the generation of a r 1 receptor pharmacophore that will enable the rational design of increasingly selective and potent r 1 ligands for probing r 1 receptor function.","publication_date":{"day":21,"month":8,"year":2012,"errors":{}},"grobid_abstract_attachment_id":43207882},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608434/A_%CF%831_receptor_pharmacophore_derived_from_a_series_of_N_substituted_4_azahexacyclo_5_4_1_0_2_6_0_3_10_0_5_9_0_8_11_dodecan_3_ols_AHDs_","translated_internal_url":"","created_at":"2016-02-29T10:07:52.077-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577293,"work_id":22608434,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"A σ1 receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs)"}],"downloadable_attachments":[{"id":43207882,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207882/thumbnails/1.jpg","file_name":"2012_-_BMCL_-_AHDs.pdf","download_url":"https://www.academia.edu/attachments/43207882/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"A_1_receptor_pharmacophore_derived_from.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207882/2012_-_BMCL_-_AHDs-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DA_1_receptor_pharmacophore_derived_from.pdf\u0026Expires=1732999529\u0026Signature=eVAFe49ApXJ8DHGIcHQ5hqQGv6-V4HjHIULD9tXbkQSdHwoWuDN6tHxoPFEnbIa-l7CPk7H8fcd4bUiOkunppmoR40bQ7uuWP1vZz8VvIOFC8iiMoZE-nbJgmhRGDEmySHlI-pQL02xn1kzhP4-ZSSdcMTDeE3J9qgZ1kkJm25vVUdSIm3eJ024tAlTEauYXGyzSwo1h7pq-aSIbpoBNpWtq~vH2gXBSEmDZWEYD~dx-44zahQyOns8BpiRJqi82LBI8gC8A6R5pKEBDUbFGHyLPAs5u-meap~KgMeNjybiezyiw1LlyBryhynYRtOXEUxdSw0dXG21PbP9cNs66qg__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"A_σ1_receptor_pharmacophore_derived_from_a_series_of_N_substituted_4_azahexacyclo_5_4_1_0_2_6_0_3_10_0_5_9_0_8_11_dodecan_3_ols_AHDs_","translated_slug":"","page_count":6,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207882,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207882/thumbnails/1.jpg","file_name":"2012_-_BMCL_-_AHDs.pdf","download_url":"https://www.academia.edu/attachments/43207882/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"A_1_receptor_pharmacophore_derived_from.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207882/2012_-_BMCL_-_AHDs-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DA_1_receptor_pharmacophore_derived_from.pdf\u0026Expires=1732999529\u0026Signature=eVAFe49ApXJ8DHGIcHQ5hqQGv6-V4HjHIULD9tXbkQSdHwoWuDN6tHxoPFEnbIa-l7CPk7H8fcd4bUiOkunppmoR40bQ7uuWP1vZz8VvIOFC8iiMoZE-nbJgmhRGDEmySHlI-pQL02xn1kzhP4-ZSSdcMTDeE3J9qgZ1kkJm25vVUdSIm3eJ024tAlTEauYXGyzSwo1h7pq-aSIbpoBNpWtq~vH2gXBSEmDZWEYD~dx-44zahQyOns8BpiRJqi82LBI8gC8A6R5pKEBDUbFGHyLPAs5u-meap~KgMeNjybiezyiw1LlyBryhynYRtOXEUxdSw0dXG21PbP9cNs66qg__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854371,"url":"http://dx.doi.org/10.1016/j.bmcl.2012.08.046"}]}, dispatcherData: dispatcherData }); 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The heterogeneous but wide distribution of s 1 in the brain has prompted the development of selective radiotracers for imaging these sites using positron emission tomography (PET). To date, some 50 carbon-11-labelled and fluorine-18-labelled candidate PET radioligands targeting s receptors have been reported. The historical development of selective s 1 receptor ligands as potential PET imaging agents, as well as the radiochemistry and application of the most recently developed examples, is described herein.","publication_date":{"day":24,"month":4,"year":2013,"errors":{}},"grobid_abstract_attachment_id":43207890},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608429/The_development_of_radiotracers_for_imaging_sigma_%CF%83_receptors_in_the_central_nervous_system_CNS_using_positron_emission_tomography_PET_","translated_internal_url":"","created_at":"2016-02-29T10:07:52.059-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577314,"work_id":22608429,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"The development of radiotracers for imaging sigma (σ) receptors in the central nervous system (CNS) using positron emission tomography (PET)"}],"downloadable_attachments":[{"id":43207890,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207890/thumbnails/1.jpg","file_name":"2013_-_JLCR_-_Sigma_radiochem.pdf","download_url":"https://www.academia.edu/attachments/43207890/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"The_development_of_radiotracers_for_imag.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207890/2013_-_JLCR_-_Sigma_radiochem-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DThe_development_of_radiotracers_for_imag.pdf\u0026Expires=1732999529\u0026Signature=YaFK~FlnxhFq0WQ3UPIGo1kffsx8gBV3JjcvopIUvKdVuIOPXukrl1nzkLwSGM613Sd7KLalNnfb6WtT3X4irQbJb6~K6~5Xr~LrcAbWXScAxP6yZ3T4pi73Zp7uIMIE~7a2IDuNFIdH3C5dbnKdlVFUM~M~CKB1J21JHa7TOkd~XpANBcnAOqhr8rdF6Ka-8cSzdr4YyAdAfElpde3x-pjjRZD4GhNDcH2Ey7E3UAiHcsjxnjrOSekuSiGk2HuOC3IREOUcuveBdrEy9tdVVmN5gj8lT7SYGWMbroQ7UTu6fmGZ4NFDq5Yv1f2cb~d0zq-FfTGoZ78ENO6VQ-6vAA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"The_development_of_radiotracers_for_imaging_sigma_σ_receptors_in_the_central_nervous_system_CNS_using_positron_emission_tomography_PET_","translated_slug":"","page_count":10,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207890,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207890/thumbnails/1.jpg","file_name":"2013_-_JLCR_-_Sigma_radiochem.pdf","download_url":"https://www.academia.edu/attachments/43207890/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"The_development_of_radiotracers_for_imag.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207890/2013_-_JLCR_-_Sigma_radiochem-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DThe_development_of_radiotracers_for_imag.pdf\u0026Expires=1732999529\u0026Signature=YaFK~FlnxhFq0WQ3UPIGo1kffsx8gBV3JjcvopIUvKdVuIOPXukrl1nzkLwSGM613Sd7KLalNnfb6WtT3X4irQbJb6~K6~5Xr~LrcAbWXScAxP6yZ3T4pi73Zp7uIMIE~7a2IDuNFIdH3C5dbnKdlVFUM~M~CKB1J21JHa7TOkd~XpANBcnAOqhr8rdF6Ka-8cSzdr4YyAdAfElpde3x-pjjRZD4GhNDcH2Ey7E3UAiHcsjxnjrOSekuSiGk2HuOC3IREOUcuveBdrEy9tdVVmN5gj8lT7SYGWMbroQ7UTu6fmGZ4NFDq5Yv1f2cb~d0zq-FfTGoZ78ENO6VQ-6vAA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854290,"url":"http://dx.doi.org/10.1002/jlcr.3010"}]}, dispatcherData: dispatcherData }); 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Adamantyl hemiaminals 9-15 displayed generally low affinity for both r 1 (K i values = 294-1950 nM) and r 2 receptors (K i values = 201-1020 nM), and negligible affinity for 42 other CNS proteins. Deoxygenation of 9-15 to give the corresponding achiral azaadamantanes 23-29 greatly improved affinity for r 1 (K i values = 8.3-239 nM) and r 2 receptors (K i values = 34-312 nM).","publication_date":{"day":14,"month":7,"year":2011,"errors":{}},"grobid_abstract_attachment_id":43207880},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608426/N_Arylalkyl_2_azaadamantanes_as_cage_expanded_polycarbocyclic_sigma_%CF%83_receptor_ligands","translated_internal_url":"","created_at":"2016-02-29T10:07:52.045-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577315,"work_id":22608426,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (σ) receptor ligands"}],"downloadable_attachments":[{"id":43207880,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207880/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Aza-adamantanes.pdf","download_url":"https://www.academia.edu/attachments/43207880/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"N_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207880/2011_-_BMCL_-_Aza-adamantanes-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DN_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf\u0026Expires=1732999529\u0026Signature=SMEGHavnmuSmA78r5Op6NSGnwKKIZXd6~lrzUIndDplEG8pABb1eIhUeQ9y2bORO1FfFXIhhYl1fqJJt~w~TLlaptUqfVKX~sGo-dGQS6NRlyHS7xmRZ-LLZKiKTlakVpziT7sd7awZU6xa30wqcygSG6Eck0-NGEDBChObFRdN7PTb2f8FJXPYkRiWNWrJMdnKIpt72g9UjuA-Q7r7SU5JpmdWL2z6qewQFrmzcUAJW6XK9GPVVtGrB~wz8qdlCQK3HVrYOZKJr6D9HlJgRjX5G0SzfAowuKNYyrkkL8iHgHVkYi3lq0unH0oqUYRp7zpi3JImjyLo46IDManPmPw__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"N_Arylalkyl_2_azaadamantanes_as_cage_expanded_polycarbocyclic_sigma_σ_receptor_ligands","translated_slug":"","page_count":4,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207880,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207880/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Aza-adamantanes.pdf","download_url":"https://www.academia.edu/attachments/43207880/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"N_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207880/2011_-_BMCL_-_Aza-adamantanes-libre.pdf?1456769283=\u0026response-content-disposition=attachment%3B+filename%3DN_Arylalkyl_2_azaadamantanes_as_cage_exp.pdf\u0026Expires=1732999529\u0026Signature=SMEGHavnmuSmA78r5Op6NSGnwKKIZXd6~lrzUIndDplEG8pABb1eIhUeQ9y2bORO1FfFXIhhYl1fqJJt~w~TLlaptUqfVKX~sGo-dGQS6NRlyHS7xmRZ-LLZKiKTlakVpziT7sd7awZU6xa30wqcygSG6Eck0-NGEDBChObFRdN7PTb2f8FJXPYkRiWNWrJMdnKIpt72g9UjuA-Q7r7SU5JpmdWL2z6qewQFrmzcUAJW6XK9GPVVtGrB~wz8qdlCQK3HVrYOZKJr6D9HlJgRjX5G0SzfAowuKNYyrkkL8iHgHVkYi3lq0unH0oqUYRp7zpi3JImjyLo46IDManPmPw__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854410,"url":"http://dx/doi.org/10.1016/j.bmcl.2011.07.028"}]}, dispatcherData: dispatcherData }); 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Radiofluorination of the appropriate tosylate precursor furnished [ 18 F]6 with a specific activity of 45 GBq/lmol, in an average radiochemical yield of 18% and greater than 98% radiochemical purity. Micro-PET imaging in Papio hamadryas baboon brain revealed [ 18 F]6 uptake consistent with r receptor distribution, and specificity for r receptors was demonstrated in a haloperidol pre-treated animal. [ 18 F]6 possesses suitable properties for PET imaging of r 1 receptors, and further investigation of this r 1 receptor tracer is warranted.","publication_date":{"day":13,"month":9,"year":2011,"errors":{}},"grobid_abstract_attachment_id":43207887},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608430/Synthesis_and_in_vivo_evaluation_of_18F_N_2_benzofuranylmethyl_N_4_2_fluoroethoxy_benzyl_piperazine_a_novel_%CF%831_receptor_PET_imaging_agent","translated_internal_url":"","created_at":"2016-02-29T10:07:52.059-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577312,"work_id":22608430,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent"},{"id":16577313,"work_id":22608430,"tagging_user_id":44167404,"tagged_user_id":null,"co_author_invite_id":1813629,"email":"s***e@sydney.edu.au","display_order":4194304,"name":"Steven Meikle","title":"Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N'-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ1 receptor PET imaging agent"}],"downloadable_attachments":[{"id":43207887,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207887/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Sigma_piperazine_PET_ligand.pdf","download_url":"https://www.academia.edu/attachments/43207887/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Synthesis_and_in_vivo_evaluation_of_18F.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207887/2011_-_BMCL_-_Sigma_piperazine_PET_ligand-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3DSynthesis_and_in_vivo_evaluation_of_18F.pdf\u0026Expires=1732999529\u0026Signature=C7gI2Hob~PrNc1-5zbxEwuB99VMSphAMGJiCYwIdX~qNyEpl5HF2G1KWIRwTwcztEQmc1L4p3l9jFBRTR7sJilSp2WkEWNwi4IEuwwHDbmilvc-bNbMKBLrPCMRROgh9I~v5nlloQSpbayDpOYbeZalzYINB5xMvc9tGLTWiLNIJes7-S2rGGTI8l7UoCUrGDU-Wiy6i7-apwVoAYQukLP9D1VqZCUi3PTaSEYtCF6aItU4cgpgOSN5FF~pF~lPl3vD7TFph~LJIMms6CiMwvKrMibgJlJc5mYgdJ7QwJ8xJ-YcZPDwiyX~PLzS0QTNWO01q2-Z9lPNR7cgRttldRQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Synthesis_and_in_vivo_evaluation_of_18F_N_2_benzofuranylmethyl_N_4_2_fluoroethoxy_benzyl_piperazine_a_novel_σ1_receptor_PET_imaging_agent","translated_slug":"","page_count":4,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207887,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207887/thumbnails/1.jpg","file_name":"2011_-_BMCL_-_Sigma_piperazine_PET_ligand.pdf","download_url":"https://www.academia.edu/attachments/43207887/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Synthesis_and_in_vivo_evaluation_of_18F.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207887/2011_-_BMCL_-_Sigma_piperazine_PET_ligand-libre.pdf?1456769282=\u0026response-content-disposition=attachment%3B+filename%3DSynthesis_and_in_vivo_evaluation_of_18F.pdf\u0026Expires=1732999529\u0026Signature=C7gI2Hob~PrNc1-5zbxEwuB99VMSphAMGJiCYwIdX~qNyEpl5HF2G1KWIRwTwcztEQmc1L4p3l9jFBRTR7sJilSp2WkEWNwi4IEuwwHDbmilvc-bNbMKBLrPCMRROgh9I~v5nlloQSpbayDpOYbeZalzYINB5xMvc9tGLTWiLNIJes7-S2rGGTI8l7UoCUrGDU-Wiy6i7-apwVoAYQukLP9D1VqZCUi3PTaSEYtCF6aItU4cgpgOSN5FF~pF~lPl3vD7TFph~LJIMms6CiMwvKrMibgJlJc5mYgdJ7QwJ8xJ-YcZPDwiyX~PLzS0QTNWO01q2-Z9lPNR7cgRttldRQ__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854375,"url":"http://dx.doi.org/10.1016/j.bmcl.2011.09.028"}]}, dispatcherData: dispatcherData }); 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Agents such as the clinical oncology tracer 2-[ 18 F]fluoro-2-deoxy-Dglucose ([ 18 F]FDG), the most widely used PET-radiopharmaceutical, are driving an increasing interest in the chemistry of radiopharmaceuticals utilizing fluorine-18. This review outlines the methods for production of fluorine-18, and the development of agents for performing radiofluorination reactions. With a few exceptions, radiofluorinations can be classified as either electrophilic or nucleophilic. The electrophilic reactions mainly use molecular [ 18 F]fluorine of moderately low specific radioactivity, or reagents prepared from it, and include additions to alkenes, reactions with carbanions and especially fluorodehydrogenation and fluorodemetallation. The nucleophilic reactions usually involve no-carrier-added (highspecific-radioactivity) [ 18 F]fluoride as its K[ 18 F]F-K 222 complex and include S N 2-type substitutions in the aliphatic series and S N Ar-type substitutions in the aromatic and heteroaromatic series. Key examples from each class of radiofluorination reaction will be described, highlighting the potential of this radioisotope in the design and preparation of fluorine-18labeled probes for PET imaging.","publication_date":{"day":null,"month":null,"year":2010,"errors":{}},"grobid_abstract_attachment_id":43207874},"translated_abstract":null,"internal_url":"https://www.academia.edu/22608433/Fluorine_18_Chemistry_for_PET_A_Concise_Introduction","translated_internal_url":"","created_at":"2016-02-29T10:07:52.066-08:00","preview_url":null,"current_user_can_edit":null,"current_user_is_owner":null,"owner_id":44167404,"coauthors_can_edit":true,"document_type":"paper","co_author_tags":[{"id":16577294,"work_id":22608433,"tagging_user_id":44167404,"tagged_user_id":36408679,"co_author_invite_id":null,"email":"m***u@sydney.edu.au","affiliation":"The University of Sydney","display_order":0,"name":"Michael Kassiou","title":"Fluorine-18 Chemistry for PET: A Concise Introduction"},{"id":16577295,"work_id":22608433,"tagging_user_id":44167404,"tagged_user_id":48835427,"co_author_invite_id":429660,"email":"f***e@cea.fr","display_order":4194304,"name":"Frédéric Dollé","title":"Fluorine-18 Chemistry for PET: A Concise Introduction"}],"downloadable_attachments":[{"id":43207874,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207874/thumbnails/1.jpg","file_name":"2010_-_CurrRadiopharm_-_F18_for_PET_intro_review.pdf","download_url":"https://www.academia.edu/attachments/43207874/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Fluorine_18_Chemistry_for_PET_A_Concise.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207874/2010_-_CurrRadiopharm_-_F18_for_PET_intro_review-libre.pdf?1456769258=\u0026response-content-disposition=attachment%3B+filename%3DFluorine_18_Chemistry_for_PET_A_Concise.pdf\u0026Expires=1732999529\u0026Signature=dlm1mqDYRok1wJrhsWIeMgyYpijeLQQvZv10FbeSqI3KzKCPbnxkU6PgWS7RNVRYiY3oP25uZfNbv-CPOuNng6j9uzg1bCINkCRt3RhVH6yeIpl~te3yWJ5E86jmb91YxFIWFW7VDJZmWFUzIojdWHeS5RjzAl5Ej7agLsa8mNj6d2bdBYoAfzZN4yPg-nkLEpdew8nzrunMEqNFqqwS-hhuPUXcmKsCwmdkj3I86bByWUIrddUBiJrcDZsZwGE~8FoERXjsgWBlhePCsyXqIxRNcK3IMEP-HiMBova0grViJYWe-tnd2vx3Gf1M57gkTJkkKxfOQCO11PISDxToaA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"slug":"Fluorine_18_Chemistry_for_PET_A_Concise_Introduction","translated_slug":"","page_count":13,"language":"en","content_type":"Work","owner":{"id":44167404,"first_name":"Samuel","middle_initials":"","last_name":"Banister","page_name":"SamuelBanister","domain_name":"stanford","created_at":"2016-02-29T10:06:07.981-08:00","display_name":"Samuel Banister","url":"https://stanford.academia.edu/SamuelBanister"},"attachments":[{"id":43207874,"title":"","file_type":"pdf","scribd_thumbnail_url":"https://attachments.academia-assets.com/43207874/thumbnails/1.jpg","file_name":"2010_-_CurrRadiopharm_-_F18_for_PET_intro_review.pdf","download_url":"https://www.academia.edu/attachments/43207874/download_file?st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&st=MTczMjk5NTkyOSw4LjIyMi4yMDguMTQ2&","bulk_download_file_name":"Fluorine_18_Chemistry_for_PET_A_Concise.pdf","bulk_download_url":"https://d1wqtxts1xzle7.cloudfront.net/43207874/2010_-_CurrRadiopharm_-_F18_for_PET_intro_review-libre.pdf?1456769258=\u0026response-content-disposition=attachment%3B+filename%3DFluorine_18_Chemistry_for_PET_A_Concise.pdf\u0026Expires=1732999529\u0026Signature=dlm1mqDYRok1wJrhsWIeMgyYpijeLQQvZv10FbeSqI3KzKCPbnxkU6PgWS7RNVRYiY3oP25uZfNbv-CPOuNng6j9uzg1bCINkCRt3RhVH6yeIpl~te3yWJ5E86jmb91YxFIWFW7VDJZmWFUzIojdWHeS5RjzAl5Ej7agLsa8mNj6d2bdBYoAfzZN4yPg-nkLEpdew8nzrunMEqNFqqwS-hhuPUXcmKsCwmdkj3I86bByWUIrddUBiJrcDZsZwGE~8FoERXjsgWBlhePCsyXqIxRNcK3IMEP-HiMBova0grViJYWe-tnd2vx3Gf1M57gkTJkkKxfOQCO11PISDxToaA__\u0026Key-Pair-Id=APKAJLOHF5GGSLRBV4ZA"}],"research_interests":[],"urls":[{"id":6854424,"url":"http://dx.doi.org/10.2174/1874471011003020068"}]}, dispatcherData: dispatcherData }); 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The use of NMDA antagonists as therapeutic agents has been restricted as a result of unwanted side effects including hallucinations and loss of co-ordination. NR2B subtype selective antagonists have previously shown a therapeutic effect without causing the side effects of broad spectrum NMDA antagonists. Considerable research has since been devoted to the development of orally bioavailable, selective NR2B antagonists and their applications in various neurological diseases. The improved therapeutic index of these compounds is expected to be the result of the subtype selectivity and cellular location of the NR2B receptors within the CNS. 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Affinities of these ligands for r 1 and r 2 receptors were investigated by means of radioligand binding assays, with the identification of N-(2-benzofuranylmethyl)-N 0 -[3-(4-methoxyphenyl)propyl]piperazine (29, K i = 3.1 nM, r 2 /r 1 = 45) as a selective r 1 ligand. The r 1 affinities and subtype selectivities of piperazines 16-21 and 26-31 were generally comparable to the corresponding benzylic analogs. 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