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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">==Tüübid== ===Võistlev=== [[võistlev antagonist|Võistlevad antagonistid]] (teatud ka kui ületavad antagonistid) seonduvad pöördumatult samale seondumissaidile (aktiivsele saidile), ilma retseptorit aktiveerimata, kus on endogeene ligand või agonist. Agonistid ja antagonistid võistlevad sama seondumisaidi pärast retseptoril. Kord seostunud antagonist blokeerib agonisti seondumist. Aktiivsuse taset retseptoril saab määrata suhtelise afiinuse ning kontsentratsiooniga igas molekulis, mis asuvad sel konkreetsel saidil. Kõrge kontsentratsioonitase võistleval agonistil suurendab retseptori pinda, mida agonist hõivab<ref name="Swinney2004" />. Antagonisti kõrgemad kontsentratsioonid on vajalikud selleks, et hoida võistlevatel antagonistidel seda hõivatuse taset seondumissaidil, mida kasutatakse. Funktsionaalsetes proovides vaadeldakse paralleelselt parempoolsete doos-vastus kurve, kus ei tohi olla maksimaalse vastuse muutust<ref name="Vauquelin2002" />. [[Interleukiin-1]] retseptori antagonist IL-1Ra on üks näide võistlevast antagonistist<ref name="pmid8379462" />. Võistleva antagonisti efekte võib alla suruda, tõstes agonisti kontsentratsiooni. Tihti (kuid mitte alati) omavad need antagonistid oma agonisti omaga väga sarnast keemilist struktuuri. ===Mittevõistlev=== Terminit ''mittevõistlev antagonist'' (kutsutakse ka mitteületavaks antagonistiks) võidakse kasutada, et kirjeldada kaht omavahelist fenomeni: ühes, kus antagonist seondub retseptori seondumissaidile, teises, kus antagonist seob end [[allosteeriline|allosteerilisele]] saidile<ref name="Golan25" />. Kuigi nende kahe fenomeni mehhanism on erinev, kutsutakse mõlemaid ''mittevõistevaiks'', sellepärast et lõppetulemus on üpris sarnane. Erinevalt võistlevatest antagonistidest, mis mõjutavad agonisti taseme suurust, et saavutada maksimaalne vastus, kuid ei mõjuta maksimaalvastuse magnituudi, ''mittevõitlevad agonistid'' vähendavad selle maksimum-vastuse magnituudi, mille võib omandada ükskõik millise hulgaga agonist. See omadus teenib neile nime ''mittevõistlev'', sest ükskõik kui palju agoniste on olemas, nende efekte ei saa teha olematuks. Mittevõistlevate agonistide funktsionaalsetes proovides toimub agonisti maksimaalvastuse doos-vastus kurvil langus ja mõnedel juhtudel on parempoone kalle olemas<ref name="Vauquelin2002" />. Parempoolne kalle on retseptori reservi olemasolul ja agonisti vastuse inhibatsioon toimub ainult, kui reserv<ref name="stephanson" /> on ammendatud. Antagonist, mis seob end retseptori aktiivsele saidile on ''mittevõistlev'' ainult siis, kui side aktiivsaidi ja antagonisti vahel on pöördumatu või sellele ligilähedane.<ref name="Golan25" />. ''Mittevõistleva'' termini kasutusala ei ole siiski ideaalne, kuna terminit "pöördumatu võistlev antagonism" võib kasutada ka kirjeldamaks sedasama fenomeni ilma, et tekiks segadus teise "mittevõistleva antagonismi" vahel, mida kirjeldatakse allpool. ''Mittevõistleva antagonisti'' teine vorm toimub allosteerilises saidis. Need antagonistid seovad täiesti erineval saidil antagonististe, kasutades teist seondumissaiti. Nad ei võistle agonistidega seondumissaidi pärast. Need antagonistid, mis on seondunud, võivad ennetada konformatsioonilisi muutusi retseptoril, mis on vajalikud pärast seda, kui agonist on seondunud aktivatsioonisaidile<ref name="Golan" />. ===Konkurentsivõimetu=== Konkurentsivõimetud antagonistid eristuvad mittevõistlevatest antagonistidest selle poolest, et nemad vajavad agonisti poolt retseptori aktivatsiooni enne, kui nad seonduvad erinevatele allosteerilistele seondumisaitidele. Seda tüüpi antagonistid toodavad sellise kineetilise profiili, kus sama hulk antagoniste blokeerivad kõrgema kontsentratsiooniga agoniste paremini kui madalama kontsentratsiooniga agoniste<ref name="Lipton" />. Memantiin, mida kasutatakse [[Alzheimeri tõbi|Alzheimeri tõve]] ravimina, on samuti konkurentsivõimetu antagonist [[NMDA retseptor]]il<ref name="Parsons" />. ===Vaikne antagonist=== Vaiksed antagonistid on võistlevad retseptor-antagonistid, millel on null-tõhusus, et aktiveerida retseptorit. Nad on nii-öelda õiged antagonistid. See termin loodi, et eristada täielikult inaktiivseid antagoniste nõrkadest [[osaline antagonist|osalistest agonistidest]] või [[inventeeritud antagonist|pöördagonistidest]]. </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=5&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-6df7948d6c-kvrvd","wgBackendResponseTime":180,"wgPageParseReport":{"limitreport":{"cputime":"0.005","walltime":"0.006","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-6df7948d6c-kvrvd","timestamp":"20241127171735","ttl":2592000,"transientcontent":false}}});});</script> </body> </html>