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data-unpinned-container-id="vector-appearance-unpinned-container" > <div class="vector-pinnable-header-label">Ilme</div> <button class="vector-pinnable-header-toggle-button vector-pinnable-header-pin-button" data-event-name="pinnable-header.vector-appearance.pin">vii külgpaanile</button> <button class="vector-pinnable-header-toggle-button vector-pinnable-header-unpin-button" data-event-name="pinnable-header.vector-appearance.unpin">peida</button> </div> </div> </div> </nav> </div> </div> <div id="bodyContent" class="vector-body" aria-labelledby="firstHeading" data-mw-ve-target-container> <div class="vector-body-before-content"> <div class="mw-indicators"> </div> </div> <div id="contentSub"><div id="mw-content-subtitle">← <a href="/wiki/Antagonist_(farmakoloogia)" title="Antagonist (farmakoloogia)">Antagonist (farmakoloogia)</a></div></div> <div id="mw-content-text" class="mw-body-content"><p>Sul pole lubatud seda lehekülge muuta järgmisel põhjusel: </p> <div class="permissions-errors"><div class="mw-permissionerror-globalblocking-blockedtext-range"><b>Sinu IP-aadress on vahemikus, mis on <a href="https://meta.wikimedia.org/wiki/Special:MyLanguage/Global_blocks" class="extiw" title="m:Special:MyLanguage/Global blocks">blokeeritud kõigis Wikimedia Foundationi vikides</a>.</b> <p>Blokeerija: <a href="/wiki/Kasutaja:Jon_Kolbert" title="Kasutaja:Jon Kolbert">‪Jon Kolbert‬</a>. Põhjus: <i><a href="https://meta.wikimedia.org/wiki/Special:MyLanguage/NOP" class="extiw" title="m:Special:MyLanguage/NOP">Open proxy/Webhost</a>: See the <a href="https://meta.wikimedia.org/wiki/WM:OP/H" class="extiw" title="m:WM:OP/H">help page</a> if you are affected </i>. </p> <ul><li>Blokeeringu algusaeg: 27. august 2023, kell 17:12</li> <li>Blokeeringu aegumistähtaeg: 27. august 2028, kell 17:12</li></ul> <p>Sinu praegune IP-aadress on 8.222.208.146. Blokeeritud vahemik on 8.222.128.0/17. </p><p>Palun lisa kõik need andmed igale järelepärimisele, mida kavatsed teha. Kui usud, et sind on blokeeritud ekslikult, leiad lisateavet ja juhised <a href="https://meta.wikimedia.org/wiki/Special:MyLanguage/No_open_proxies" class="extiw" title="m:Special:MyLanguage/No open proxies">avatud prokside keelamist</a> puudutavast globaalsest reeglistikust. </p> Muul juhul <a href="https://meta.wikimedia.org/wiki/Steward_requests/Global" class="extiw" title="m:Steward requests/Global">postita palun blokeeringu arutamiseks palve</a>, mis metavikis üle vaadatakse. Saad ka saata <a href="https://meta.wikimedia.org/wiki/Special:MyLanguage/Stewards" class="extiw" title="m:Special:MyLanguage/Stewards">stjuuarditele</a> <a href="https://meta.wikimedia.org/wiki/Special:MyLanguage/VRT" class="extiw" title="m:Special:MyLanguage/VRT">VRT</a>-süsteemi aadressile <kbd>stewards@wikimedia.org</kbd> kirja, millele on lisatud kõik ülaltoodud üksikasjad.</div></div><hr /> <p>Saad vaadata ja kopeerida selle lehekülje lähteteksti. </p><textarea readonly="" accesskey="," id="wpTextbox1" cols="80" rows="25" style="" class="mw-editfont-monospace" lang="et" dir="ltr" name="wpTextbox1">==Farmakodünaamika== {{Main|Farmakodünaamika}} ===Efektiivsus ja potentsiaalsus=== Definitsiooni järgi ei ole antagonistidel mingit mõju, et aktiveerida neid retseptoreid, millega nad seonduvad. Kuigi antagonistid ei hoia retseptori aktiveerimisvõimet, inhibeerivad nad ühekorra seondudes agonisti, inventeeritud agonisti ja [[osaline agonist|osalise agonisti]] funktsiooni. Funktsionaalsetes antagonistiproovides mõõdab [[Doos-vastus seos|doos-vastus kurv]] erinevatel kontsentratsioonidel antagonistide efekti võimet, kus nad suudavad pöörata ümber agonisti aktiivsust<ref name="2006Kenakin" />. Antagonisti potentsiaali mõõdetakse tema [[IC50|IC<sub>50</sub>]] väärtusega. Seda saab antud antagonisti kohta välja arvutada, saades teada tema kontsentratsiooni, mis on vajalik, et inhibeerida pool agonisti maksimaalsest bioloogilisest vastusest. Madalama kontsentratsiooniga ravimeid võib seostada vähemate või väiksemate kõrvaltoimetega<ref name="Swinney2004" />. ===Afiinsus=== Antagonisti ja [[seondumissait|seondumissaidi]] afiinsus (K<sub>i</sub>), <math> K_i = \frac{IC_{50}}{1+\frac{[S]}{K_m}} </math> retseptori seostumise võime, määrab agonisti inhibeerimise aja. Antagonisti afiinsust võib määrata eksperimentaalselt, kasutades [[Schildi regressioon]]i või [[Cheng-Prusoffi võrrand]]it võistlevate antagonistide [[radioligand]]ide seondumiste uurimiseks. Schildi regressiooni saab kasutada selgitamaks antagonistide olemust, et kas ollakse alguses võistlev või mittevõistlev ja Ki determinatsioon on sõltumatu kasutusel oleva agonisti afiinsusest, tõhususest või kontsentratsioonist. Siiski on tähtis, et tasakaal oleks saavutatud. Retseptori tasakaalu jõudmisel tuleb võtta arvesse tunnetuse vähenemist. Antagonisti afiinsuse konstanti, mis omab kahte või enamat efekti, nagu näiteks neuromuskulaar-blokeerivad agendid, mis blokeerivad samuti ioonkanaleid ning antagoniseerivad antagonistide sidumisvõimet, ei saa analüüsida kasutades Scildi regressiooni<ref name="Wyllie" /><ref name="Colquhoun" />. Schildi regressioon seisneb doosi suhte muutumises – doos-vastus kurvil võrreldakse agonisti ja olemasoleva võistleva antagonisti EC<sub>50</sub> suhet. Kasutatava antagonisti proovi suurendamine võib mõjutada doosi suhet. Afiinsus või K<sub>i</sub> on see, kus sirge lõikab regressioonianalüüsil x-telge. Samas Schildi regressiooniga agonisti kontsentratsioon varieerub, kui kasutatakse Chengi-Prusoffi võrrandit, et saada kätte K<sub>i</sub> väärtused<ref name="Cheng" />. Cheng-Prusoffi faktor võtab arvesse seda efekti, mis juhtub, kui muuta agonisti kontsentratsiooni ja afiinsust retseptoril, millel on juba võistlev inhibeeriv antagonist peal. </textarea><div class="templatesUsed"></div><p id="mw-returnto">Naase lehele <a href="/wiki/Antagonist_(farmakoloogia)" title="Antagonist (farmakoloogia)">Antagonist (farmakoloogia)</a></p> <noscript><img src="https://login.wikimedia.org/wiki/Special:CentralAutoLogin/start?type=1x1" alt="" width="1" height="1" style="border: none; position: absolute;"></noscript> <div class="printfooter" data-nosnippet="">Pärit leheküljelt "<a dir="ltr" href="https://et.wikipedia.org/wiki/Antagonist_(farmakoloogia)">https://et.wikipedia.org/wiki/Antagonist_(farmakoloogia)</a>"</div></div> <div id="catlinks" class="catlinks catlinks-allhidden" data-mw="interface"></div> </div> </main> </div> <div class="mw-footer-container"> <footer id="footer" class="mw-footer" > <ul id="footer-info"> </ul> <ul id="footer-places"> <li id="footer-places-privacy"><a href="https://foundation.wikimedia.org/wiki/Special:MyLanguage/Policy:Privacy_policy">Andmekaitsepõhimõtted</a></li> <li id="footer-places-about"><a href="/wiki/Vikipeedia:Tiitelandmed">Tiitelandmed</a></li> <li id="footer-places-disclaimers"><a href="/wiki/Vikipeedia:%C3%9Cldine_lahti%C3%BCtlus">Lahtiütlused</a></li> <li id="footer-places-wm-codeofconduct"><a href="https://foundation.wikimedia.org/wiki/Special:MyLanguage/Policy:Universal_Code_of_Conduct">Käitumisjuhis</a></li> <li id="footer-places-developers"><a href="https://developer.wikimedia.org">Arendajad</a></li> <li id="footer-places-statslink"><a href="https://stats.wikimedia.org/#/et.wikipedia.org">Arvandmed</a></li> <li id="footer-places-cookiestatement"><a href="https://foundation.wikimedia.org/wiki/Special:MyLanguage/Policy:Cookie_statement">Küpsiste avaldus</a></li> <li id="footer-places-mobileview"><a href="//et.m.wikipedia.org/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=2&mobileaction=toggle_view_mobile" class="noprint stopMobileRedirectToggle">Mobiilivaade</a></li> </ul> <ul id="footer-icons" class="noprint"> <li id="footer-copyrightico"><a href="https://wikimediafoundation.org/" class="cdx-button cdx-button--fake-button cdx-button--size-large cdx-button--fake-button--enabled"><img src="/static/images/footer/wikimedia-button.svg" width="84" height="29" alt="Wikimedia Foundation" loading="lazy"></a></li> <li id="footer-poweredbyico"><a href="https://www.mediawiki.org/" class="cdx-button cdx-button--fake-button cdx-button--size-large cdx-button--fake-button--enabled"><img src="/w/resources/assets/poweredby_mediawiki.svg" alt="Powered by MediaWiki" width="88" height="31" loading="lazy"></a></li> </ul> </footer> </div> </div> </div> <div class="vector-settings" id="p-dock-bottom"> <ul></ul> </div><script>(RLQ=window.RLQ||[]).push(function(){mw.config.set({"wgHostname":"mw-web.codfw.main-f69cdc8f6-szrlp","wgBackendResponseTime":181,"wgPageParseReport":{"limitreport":{"cputime":"0.004","walltime":"0.005","ppvisitednodes":{"value":17,"limit":1000000},"postexpandincludesize":{"value":758,"limit":2097152},"templateargumentsize":{"value":0,"limit":2097152},"expansiondepth":{"value":2,"limit":100},"expensivefunctioncount":{"value":0,"limit":500},"unstrip-depth":{"value":0,"limit":20},"unstrip-size":{"value":0,"limit":5000000},"entityaccesscount":{"value":0,"limit":400},"timingprofile":["100.00% 0.000 1 -total"]},"cachereport":{"origin":"mw-web.codfw.main-f69cdc8f6-szrlp","timestamp":"20241124000537","ttl":2592000,"transientcontent":false}}});});</script> </body> </html>