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terminivõistlus\u003C/a\u003E\u003C/b\u003E!\u003C/small\u003E\u003C/span\u003E\n\u003C/p\u003E\u003C/div\u003E\u003C/div\u003E\u003C/div\u003E\u003C/div\u003E";}}());</script></div> </div> <div class="vector-column-start"> <div class="vector-main-menu-container"> <div id="mw-navigation"> <nav id="mw-panel" class="vector-main-menu-landmark" aria-label="Sait"> <div id="vector-main-menu-pinned-container" class="vector-pinned-container"> </div> </nav> </div> </div> <div class="vector-sticky-pinned-container"> <nav id="mw-panel-toc" aria-label="Sisukord" data-event-name="ui.sidebar-toc" class="mw-table-of-contents-container vector-toc-landmark"> <div id="vector-toc-pinned-container" class="vector-pinned-container"> <div id="vector-toc" class="vector-toc vector-pinnable-element"> <div class="vector-pinnable-header vector-toc-pinnable-header vector-pinnable-header-pinned" data-feature-name="toc-pinned" data-pinnable-element-id="vector-toc" > <h2 class="vector-pinnable-header-label">Sisukord</h2> <button class="vector-pinnable-header-toggle-button vector-pinnable-header-pin-button" data-event-name="pinnable-header.vector-toc.pin">vii külgpaanile</button> <button class="vector-pinnable-header-toggle-button vector-pinnable-header-unpin-button" data-event-name="pinnable-header.vector-toc.unpin">peida</button> </div> <ul class="vector-toc-contents" id="mw-panel-toc-list"> <li id="toc-mw-content-text" class="vector-toc-list-item vector-toc-level-1"> <a href="#" class="vector-toc-link"> <div class="vector-toc-text">Algus</div> </a> </li> <li id="toc-Retseptorid" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Retseptorid"> <div class="vector-toc-text"> <span class="vector-toc-numb">1</span> <span>Retseptorid</span> </div> </a> <ul id="toc-Retseptorid-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Farmakodünaamika" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Farmakodünaamika"> <div class="vector-toc-text"> <span class="vector-toc-numb">2</span> <span>Farmakodünaamika</span> </div> </a> <button aria-controls="toc-Farmakodünaamika-sublist" class="cdx-button cdx-button--weight-quiet cdx-button--icon-only vector-toc-toggle"> <span class="vector-icon mw-ui-icon-wikimedia-expand"></span> <span>Lülita ümber alaosa "Farmakodünaamika"</span> </button> <ul id="toc-Farmakodünaamika-sublist" class="vector-toc-list"> <li id="toc-Efektiivsus_ja_potentsiaalsus" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Efektiivsus_ja_potentsiaalsus"> <div class="vector-toc-text"> <span class="vector-toc-numb">2.1</span> <span>Efektiivsus ja potentsiaalsus</span> </div> </a> <ul id="toc-Efektiivsus_ja_potentsiaalsus-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Afiinsus" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Afiinsus"> <div class="vector-toc-text"> <span class="vector-toc-numb">2.2</span> <span>Afiinsus</span> </div> </a> <ul id="toc-Afiinsus-sublist" class="vector-toc-list"> </ul> </li> </ul> </li> <li id="toc-Tüübid" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Tüübid"> <div class="vector-toc-text"> <span class="vector-toc-numb">3</span> <span>Tüübid</span> </div> </a> <button aria-controls="toc-Tüübid-sublist" class="cdx-button cdx-button--weight-quiet cdx-button--icon-only vector-toc-toggle"> <span class="vector-icon mw-ui-icon-wikimedia-expand"></span> <span>Lülita ümber alaosa "Tüübid"</span> </button> <ul id="toc-Tüübid-sublist" class="vector-toc-list"> <li id="toc-Võistlev" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Võistlev"> <div class="vector-toc-text"> <span class="vector-toc-numb">3.1</span> <span>Võistlev</span> </div> </a> <ul id="toc-Võistlev-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Mittevõistlev" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Mittevõistlev"> <div class="vector-toc-text"> <span class="vector-toc-numb">3.2</span> <span>Mittevõistlev</span> </div> </a> <ul id="toc-Mittevõistlev-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Konkurentsivõimetu" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Konkurentsivõimetu"> <div class="vector-toc-text"> <span class="vector-toc-numb">3.3</span> <span>Konkurentsivõimetu</span> </div> </a> <ul id="toc-Konkurentsivõimetu-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Vaikne_antagonist" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Vaikne_antagonist"> <div class="vector-toc-text"> <span class="vector-toc-numb">3.4</span> <span>Vaikne antagonist</span> </div> </a> <ul id="toc-Vaikne_antagonist-sublist" class="vector-toc-list"> </ul> </li> </ul> </li> <li id="toc-Viited" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#Viited"> <div class="vector-toc-text"> <span class="vector-toc-numb">4</span> <span>Viited</span> </div> </a> <ul id="toc-Viited-sublist" class="vector-toc-list"> </ul> </li> </ul> </div> </div> </nav> </div> </div> <div class="mw-content-container"> <main id="content" class="mw-body"> <header class="mw-body-header vector-page-titlebar"> <nav aria-label="Sisukord" class="vector-toc-landmark"> <div id="vector-page-titlebar-toc" class="vector-dropdown vector-page-titlebar-toc vector-button-flush-left" > <input type="checkbox" id="vector-page-titlebar-toc-checkbox" role="button" aria-haspopup="true" data-event-name="ui.dropdown-vector-page-titlebar-toc" class="vector-dropdown-checkbox " aria-label="Lülita sisukord ümber" > <label id="vector-page-titlebar-toc-label" for="vector-page-titlebar-toc-checkbox" class="vector-dropdown-label cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--icon-only " aria-hidden="true" ><span class="vector-icon mw-ui-icon-listBullet mw-ui-icon-wikimedia-listBullet"></span> <span class="vector-dropdown-label-text">Lülita sisukord ümber</span> </label> <div class="vector-dropdown-content"> <div id="vector-page-titlebar-toc-unpinned-container" class="vector-unpinned-container"> </div> </div> </div> </nav> <h1 id="firstHeading" class="firstHeading mw-first-heading"><span class="mw-page-title-main">Antagonist (farmakoloogia)</span></h1> <div id="p-lang-btn" class="vector-dropdown mw-portlet mw-portlet-lang" > <input type="checkbox" id="p-lang-btn-checkbox" role="button" aria-haspopup="true" data-event-name="ui.dropdown-p-lang-btn" class="vector-dropdown-checkbox mw-interlanguage-selector" aria-label="Mine teises keeles artiklisse. Saadaval 32 keeles" > <label id="p-lang-btn-label" for="p-lang-btn-checkbox" class="vector-dropdown-label cdx-button cdx-button--fake-button cdx-button--fake-button--enabled cdx-button--weight-quiet cdx-button--action-progressive mw-portlet-lang-heading-32" aria-hidden="true" ><span class="vector-icon mw-ui-icon-language-progressive mw-ui-icon-wikimedia-language-progressive"></span> <span class="vector-dropdown-label-text">32 keelt</span> </label> <div class="vector-dropdown-content"> <div class="vector-menu-content"> <ul class="vector-menu-content-list"> <li class="interlanguage-link interwiki-ar mw-list-item"><a href="https://ar.wikipedia.org/wiki/%D9%85%D9%86%D8%A7%D9%87%D8%B6%D8%A9_(%D8%A3%D8%AF%D9%88%D9%8A%D8%A9)" title="مناهضة (أدوية) – araabia" lang="ar" hreflang="ar" data-title="مناهضة (أدوية)" data-language-autonym="العربية" data-language-local-name="araabia" class="interlanguage-link-target"><span>العربية</span></a></li><li class="interlanguage-link interwiki-id mw-list-item"><a href="https://id.wikipedia.org/wiki/Antagonis_reseptor" title="Antagonis reseptor – indoneesia" lang="id" hreflang="id" data-title="Antagonis reseptor" data-language-autonym="Bahasa Indonesia" data-language-local-name="indoneesia" class="interlanguage-link-target"><span>Bahasa Indonesia</span></a></li><li class="interlanguage-link interwiki-bg mw-list-item"><a href="https://bg.wikipedia.org/wiki/%D0%90%D0%BD%D1%82%D0%B0%D0%B3%D0%BE%D0%BD%D0%B8%D1%81%D1%82_(%D1%84%D0%B0%D1%80%D0%BC%D0%B0%D0%BA%D0%BE%D0%BB%D0%BE%D0%B3%D0%B8%D1%8F)" title="Антагонист (фармакология) – bulgaaria" lang="bg" hreflang="bg" data-title="Антагонист (фармакология)" data-language-autonym="Български" data-language-local-name="bulgaaria" class="interlanguage-link-target"><span>Български</span></a></li><li class="interlanguage-link interwiki-ca mw-list-item"><a href="https://ca.wikipedia.org/wiki/Antagonista_(bioqu%C3%ADmica_i_farmacologia)" title="Antagonista (bioquímica i farmacologia) – katalaani" lang="ca" hreflang="ca" data-title="Antagonista (bioquímica i farmacologia)" data-language-autonym="Català" data-language-local-name="katalaani" class="interlanguage-link-target"><span>Català</span></a></li><li class="interlanguage-link interwiki-de mw-list-item"><a href="https://de.wikipedia.org/wiki/Antagonist_(Pharmakologie)" title="Antagonist (Pharmakologie) – saksa" lang="de" hreflang="de" data-title="Antagonist (Pharmakologie)" data-language-autonym="Deutsch" data-language-local-name="saksa" class="interlanguage-link-target"><span>Deutsch</span></a></li><li class="interlanguage-link interwiki-en badge-Q17437798 badge-goodarticle mw-list-item" title="hea artikkel"><a href="https://en.wikipedia.org/wiki/Receptor_antagonist" title="Receptor antagonist – inglise" lang="en" hreflang="en" data-title="Receptor antagonist" data-language-autonym="English" data-language-local-name="inglise" class="interlanguage-link-target"><span>English</span></a></li><li class="interlanguage-link interwiki-es mw-list-item"><a href="https://es.wikipedia.org/wiki/Antagonista_(bioqu%C3%ADmica)" title="Antagonista (bioquímica) – hispaania" lang="es" hreflang="es" data-title="Antagonista (bioquímica)" data-language-autonym="Español" data-language-local-name="hispaania" class="interlanguage-link-target"><span>Español</span></a></li><li class="interlanguage-link interwiki-eu mw-list-item"><a href="https://eu.wikipedia.org/wiki/Antagonista_(biokimika)" title="Antagonista (biokimika) – baski" lang="eu" hreflang="eu" data-title="Antagonista (biokimika)" data-language-autonym="Euskara" data-language-local-name="baski" class="interlanguage-link-target"><span>Euskara</span></a></li><li class="interlanguage-link interwiki-fa mw-list-item"><a href="https://fa.wikipedia.org/wiki/%D8%A2%D9%86%D8%AA%D8%A7%DA%AF%D9%88%D9%86%DB%8C%D8%B3%D8%AA_%DA%AF%DB%8C%D8%B1%D9%86%D8%AF%D9%87" title="آنتاگونیست گیرنده – pärsia" lang="fa" hreflang="fa" data-title="آنتاگونیست گیرنده" data-language-autonym="فارسی" data-language-local-name="pärsia" class="interlanguage-link-target"><span>فارسی</span></a></li><li class="interlanguage-link interwiki-fr mw-list-item"><a href="https://fr.wikipedia.org/wiki/Antagoniste_(biochimie)" title="Antagoniste (biochimie) – prantsuse" lang="fr" hreflang="fr" data-title="Antagoniste (biochimie)" data-language-autonym="Français" data-language-local-name="prantsuse" class="interlanguage-link-target"><span>Français</span></a></li><li class="interlanguage-link interwiki-ko mw-list-item"><a href="https://ko.wikipedia.org/wiki/%EC%88%98%EC%9A%A9%EC%B2%B4_%EA%B8%B8%ED%95%AD%EC%A0%9C" title="수용체 길항제 – korea" lang="ko" hreflang="ko" data-title="수용체 길항제" data-language-autonym="한국어" data-language-local-name="korea" class="interlanguage-link-target"><span>한국어</span></a></li><li class="interlanguage-link interwiki-hr mw-list-item"><a href="https://hr.wikipedia.org/wiki/Antagonist_(kemija)" title="Antagonist (kemija) – horvaadi" lang="hr" hreflang="hr" data-title="Antagonist (kemija)" data-language-autonym="Hrvatski" data-language-local-name="horvaadi" class="interlanguage-link-target"><span>Hrvatski</span></a></li><li class="interlanguage-link interwiki-is mw-list-item"><a href="https://is.wikipedia.org/wiki/Vi%C3%B0takahindri" title="Viðtakahindri – islandi" lang="is" hreflang="is" data-title="Viðtakahindri" data-language-autonym="Íslenska" data-language-local-name="islandi" class="interlanguage-link-target"><span>Íslenska</span></a></li><li class="interlanguage-link interwiki-it mw-list-item"><a href="https://it.wikipedia.org/wiki/Antagonista_(biochimica)" title="Antagonista (biochimica) – itaalia" lang="it" hreflang="it" data-title="Antagonista (biochimica)" data-language-autonym="Italiano" data-language-local-name="itaalia" class="interlanguage-link-target"><span>Italiano</span></a></li><li class="interlanguage-link interwiki-he mw-list-item"><a href="https://he.wikipedia.org/wiki/%D7%90%D7%A0%D7%98%D7%92%D7%95%D7%A0%D7%99%D7%A1%D7%98_(%D7%A4%D7%A8%D7%9E%D7%A7%D7%95%D7%9C%D7%95%D7%92%D7%99%D7%94)" title="אנטגוניסט (פרמקולוגיה) – heebrea" lang="he" hreflang="he" data-title="אנטגוניסט (פרמקולוגיה)" data-language-autonym="עברית" data-language-local-name="heebrea" class="interlanguage-link-target"><span>עברית</span></a></li><li class="interlanguage-link interwiki-arz badge-Q17437798 badge-goodarticle mw-list-item" title="hea artikkel"><a href="https://arz.wikipedia.org/wiki/%D9%85%D9%86%D8%A7%D9%87%D8%B6_%D8%A7%D9%84%D9%85%D8%B3%D8%AA%D9%82%D8%A8%D9%84" title="مناهض المستقبل – Egiptuse araabia" lang="arz" hreflang="arz" data-title="مناهض المستقبل" data-language-autonym="مصرى" data-language-local-name="Egiptuse araabia" class="interlanguage-link-target"><span>مصرى</span></a></li><li class="interlanguage-link interwiki-nl mw-list-item"><a href="https://nl.wikipedia.org/wiki/Antagonist_(biochemie)" title="Antagonist (biochemie) – hollandi" lang="nl" hreflang="nl" data-title="Antagonist (biochemie)" data-language-autonym="Nederlands" data-language-local-name="hollandi" class="interlanguage-link-target"><span>Nederlands</span></a></li><li class="interlanguage-link interwiki-ja mw-list-item"><a href="https://ja.wikipedia.org/wiki/%E5%8F%97%E5%AE%B9%E4%BD%93%E6%8B%AE%E6%8A%97%E8%96%AC" title="受容体拮抗薬 – jaapani" lang="ja" hreflang="ja" data-title="受容体拮抗薬" data-language-autonym="日本語" data-language-local-name="jaapani" class="interlanguage-link-target"><span>日本語</span></a></li><li class="interlanguage-link interwiki-pl mw-list-item"><a href="https://pl.wikipedia.org/wiki/Antagonista_(farmakologia)" title="Antagonista (farmakologia) – poola" lang="pl" hreflang="pl" data-title="Antagonista (farmakologia)" data-language-autonym="Polski" data-language-local-name="poola" class="interlanguage-link-target"><span>Polski</span></a></li><li class="interlanguage-link interwiki-pt mw-list-item"><a href="https://pt.wikipedia.org/wiki/Antagonista_(farmacologia)" title="Antagonista (farmacologia) – portugali" lang="pt" hreflang="pt" data-title="Antagonista (farmacologia)" data-language-autonym="Português" data-language-local-name="portugali" class="interlanguage-link-target"><span>Português</span></a></li><li class="interlanguage-link interwiki-ro mw-list-item"><a href="https://ro.wikipedia.org/wiki/Antagonist_(farmacologie)" title="Antagonist (farmacologie) – rumeenia" lang="ro" hreflang="ro" data-title="Antagonist (farmacologie)" data-language-autonym="Română" data-language-local-name="rumeenia" class="interlanguage-link-target"><span>Română</span></a></li><li class="interlanguage-link interwiki-ru mw-list-item"><a href="https://ru.wikipedia.org/wiki/%D0%90%D0%BD%D1%82%D0%B0%D0%B3%D0%BE%D0%BD%D0%B8%D1%81%D1%82_(%D0%B1%D0%B8%D0%BE%D1%85%D0%B8%D0%BC%D0%B8%D1%8F)" title="Антагонист (биохимия) – vene" lang="ru" hreflang="ru" data-title="Антагонист (биохимия)" data-language-autonym="Русский" data-language-local-name="vene" class="interlanguage-link-target"><span>Русский</span></a></li><li class="interlanguage-link interwiki-simple mw-list-item"><a href="https://simple.wikipedia.org/wiki/Receptor_antagonist" title="Receptor antagonist – lihtsustatud inglise" lang="en-simple" hreflang="en-simple" data-title="Receptor antagonist" data-language-autonym="Simple English" data-language-local-name="lihtsustatud inglise" class="interlanguage-link-target"><span>Simple English</span></a></li><li class="interlanguage-link interwiki-sl mw-list-item"><a href="https://sl.wikipedia.org/wiki/Antagonist_(farmakologija)" title="Antagonist (farmakologija) – sloveeni" lang="sl" hreflang="sl" data-title="Antagonist (farmakologija)" data-language-autonym="Slovenščina" data-language-local-name="sloveeni" class="interlanguage-link-target"><span>Slovenščina</span></a></li><li class="interlanguage-link interwiki-sr mw-list-item"><a href="https://sr.wikipedia.org/wiki/Antagonist_(farmakologija)" title="Antagonist (farmakologija) – serbia" lang="sr" hreflang="sr" data-title="Antagonist (farmakologija)" data-language-autonym="Српски / srpski" data-language-local-name="serbia" class="interlanguage-link-target"><span>Српски / srpski</span></a></li><li class="interlanguage-link interwiki-sh mw-list-item"><a href="https://sh.wikipedia.org/wiki/Antagonist_(farmakologija)" title="Antagonist (farmakologija) – serbia-horvaadi" lang="sh" hreflang="sh" data-title="Antagonist (farmakologija)" data-language-autonym="Srpskohrvatski / српскохрватски" data-language-local-name="serbia-horvaadi" class="interlanguage-link-target"><span>Srpskohrvatski / српскохрватски</span></a></li><li class="interlanguage-link interwiki-fi mw-list-item"><a href="https://fi.wikipedia.org/wiki/Antagonisti_(l%C3%A4%C3%A4ketiede)" title="Antagonisti (lääketiede) – soome" lang="fi" hreflang="fi" data-title="Antagonisti (lääketiede)" data-language-autonym="Suomi" data-language-local-name="soome" class="interlanguage-link-target"><span>Suomi</span></a></li><li class="interlanguage-link interwiki-sv mw-list-item"><a href="https://sv.wikipedia.org/wiki/Antagonist_(farmakologi)" title="Antagonist (farmakologi) – rootsi" lang="sv" hreflang="sv" data-title="Antagonist (farmakologi)" data-language-autonym="Svenska" data-language-local-name="rootsi" class="interlanguage-link-target"><span>Svenska</span></a></li><li class="interlanguage-link interwiki-th mw-list-item"><a href="https://th.wikipedia.org/wiki/%E0%B9%81%E0%B8%AD%E0%B8%99%E0%B8%95%E0%B8%B2%E0%B9%82%E0%B8%81%E0%B8%99%E0%B8%B4%E0%B8%AA%E0%B8%95%E0%B9%8C" title="แอนตาโกนิสต์ – tai" lang="th" hreflang="th" data-title="แอนตาโกนิสต์" data-language-autonym="ไทย" data-language-local-name="tai" class="interlanguage-link-target"><span>ไทย</span></a></li><li class="interlanguage-link interwiki-tr mw-list-item"><a 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class="hide-when-compact"></span> <small><i>(Jaanuar 2012)</i></small><span class="hide-when-compact"> <br /><small>Palun aita <a class="external text" href="https://et.wikipedia.org/w/index.php?title=Antagonist_(farmakoloogia)&action=edit">artiklit toimetada</a>.</small> <small>(<a href="/wiki/Juhend:Toimetusm%C3%A4rkuste_eemaldamine" title="Juhend:Toimetusmärkuste eemaldamine">Kuidas ja millal see märkus eemaldada?</a>)</small></span><span class="hide-when-compact"></span></div></td></tr></tbody></table> <figure class="mw-default-size" typeof="mw:File/Thumb"><a href="/wiki/Fail:Antagonist_3.png" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/8/8d/Antagonist_3.png/220px-Antagonist_3.png" decoding="async" width="220" height="186" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/8/8d/Antagonist_3.png/330px-Antagonist_3.png 1.5x, //upload.wikimedia.org/wikipedia/commons/8/8d/Antagonist_3.png 2x" data-file-width="420" data-file-height="356" /></a><figcaption>Antagonist blokeerib <a href="/wiki/Agonist" title="Agonist">agonisti</a> seondumise <a href="/wiki/Retseptor_(biokeemia)" title="Retseptor (biokeemia)">retseptormolekulil</a>, inhibeerides sellega retseptor-agonisti loodud signaali</figcaption></figure> <p><b>Retseptori antagonist</b> on <a href="/wiki/Retseptor_(biokeemia)" title="Retseptor (biokeemia)">retseptori</a> <a href="/wiki/Ligand_(biokeemia)" title="Ligand (biokeemia)">ligandi</a> tüüp või <a href="/wiki/Ravim" title="Ravim">ravim</a>, mis seostudes vaadeldava retseptoriga ei anna bioloogilist signaali, seega nõrgestab või blokeerib täielikult <a href="/wiki/Agonist" title="Agonist">agonist</a>-vahendatud toimet.<sup id="cite_ref-pharmguide_1-0" class="reference"><a href="#cite_note-pharmguide-1"><span class="cite-bracket">[</span>1<span class="cite-bracket">]</span></a></sup> Farmakoloogia seisukohalt on antagonistid keemiliselt <a href="/wiki/Afiinsus_(keemia)" class="mw-redirect" title="Afiinsus (keemia)">afiinsed</a> kindlale retseptorile, kuid kasulik efekt puudub, signaali edastamist ei toimu ning lisaks takistatakse agonisti või <a href="/w/index.php?title=Inventeeritud_agonist&action=edit&redlink=1" class="new" title="Inventeeritud agonist (pole veel kirjutatud)">pöördagonisti</a> seostumist retseptorile. <b>Antagonisti</b> toime tuleneb tema seondumisest retseptori aktiivtsentrisse, <a href="/wiki/Allosteeriline" class="mw-redirect" title="Allosteeriline">allosteerilisse</a> saiti või saiti, mis tavaliselt ei osale retseptori aktiivsuse regulatsioonis. Antagonisti mõju võib olla pöörduv või pöördumatu, sõltudes antagonisti-retseptori kompleksi elueast. Enamik ravimi antagoniste (ravimid, mille toimemehhanism on sama nagu antagonistidel) saavutavad oma efekti, konkureerides endogeensete ligandidega või substraatidega retseptori sidumissaitidele <sup id="cite_ref-pmid12209152_2-0" class="reference"><a href="#cite_note-pmid12209152-2"><span class="cite-bracket">[</span>2<span class="cite-bracket">]</span></a></sup>. Kuna antagonistid rikuvad tihti neuronite vahelise kommunikatsiooni, siis nende pikaajalist (kroonilist) kasutamist on seostatud neuronaalse surmaga. Väga tugevad antagonistid on toksilised.<sup id="cite_ref-Dorph_3-0" class="reference"><a href="#cite_note-Dorph-3"><span class="cite-bracket">[</span>3<span class="cite-bracket">]</span></a></sup>. </p> <meta property="mw:PageProp/toc" /> <div class="mw-heading mw-heading2"><h2 id="Retseptorid">Retseptorid</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=1" title="Muuda alaosa "Retseptorid"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=1" title="Muuda alaosa "Retseptorid" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <dl><dd><span typeof="mw:File"><span><img src="//upload.wikimedia.org/wikipedia/commons/thumb/a/a3/Next.svg/12px-Next.svg.png" decoding="async" width="12" height="12" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/a/a3/Next.svg/18px-Next.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/a/a3/Next.svg/24px-Next.svg.png 2x" data-file-width="160" data-file-height="160" /></span></span> <i>Pikemalt artiklis <a href="/wiki/Retseptor_(biokeemia)" title="Retseptor (biokeemia)">Retseptor (biokeemia)</a></i></dd></dl> <p>Biokeemilised retseptorid on suured <a href="/wiki/Valk" class="mw-redirect" title="Valk">valgulised</a> <a href="/wiki/Molekul" title="Molekul">molekulid</a>, mida võidakse aktiveerida ligandi seostumisega (näiteks <a href="/wiki/Hormoon" class="mw-redirect" title="Hormoon">hormoon</a> või ravim).<sup id="cite_ref-2006Kenakin_4-0" class="reference"><a href="#cite_note-2006Kenakin-4"><span class="cite-bracket">[</span>4<span class="cite-bracket">]</span></a></sup> Retseptorid võivad olla membraansed (asetsevad rakumembraanil) või <a href="/w/index.php?title=Intratsellulaarsne&action=edit&redlink=1" class="new" title="Intratsellulaarsne (pole veel kirjutatud)">intratselluraalsed</a> (<a href="/wiki/Rakutuum" title="Rakutuum">tuumal</a> ja <a href="/wiki/Mitokonder" title="Mitokonder">mitokondritel</a>). Seondumine toimub <a href="/wiki/Mittekovalentne_side" title="Mittekovalentne side">mittekovalentselt</a> seondumissaitidel retseptori ja ligandi vahel. Retseptor võib sisaldada ühte või mitut ligandide seondumisaiti. Seondumine retseptori aktiivsele või allosteerilisele saidile reguleerib otseselt tema aktivatsiooni.<sup id="cite_ref-2006Kenakin_4-1" class="reference"><a href="#cite_note-2006Kenakin-4"><span class="cite-bracket">[</span>4<span class="cite-bracket">]</span></a></sup>.<sup id="cite_ref-May_5-0" class="reference"><a href="#cite_note-May-5"><span class="cite-bracket">[</span>5<span class="cite-bracket">]</span></a></sup> Antagonistid saavutavad oma tulemuse läbi retseptorite vastastikmõjude, hoides ära agonist-indutseeritud vastuseid. Seda saavutatakse seondudes aktiivsetele või allosteerilistele saitidele.<sup id="cite_ref-Christopoulos_6-0" class="reference"><a href="#cite_note-Christopoulos-6"><span class="cite-bracket">[</span>6<span class="cite-bracket">]</span></a></sup> Lisaks sellele võivad antagonistid toimida unikaalsetel seondumissaitidel, mis tavaliselt ei osale retseptorite bioloogilisel regulatsioonil<sup id="cite_ref-Christopoulos_6-1" class="reference"><a href="#cite_note-Christopoulos-6"><span class="cite-bracket">[</span>6<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Bleicher_7-0" class="reference"><a href="#cite_note-Bleicher-7"><span class="cite-bracket">[</span>7<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Rees_8-0" class="reference"><a href="#cite_note-Rees-8"><span class="cite-bracket">[</span>8<span class="cite-bracket">]</span></a></sup>. </p><p>Termin <i>antagonist</i> oli algselt mõeldud selleks, et kirjeldada narkootiliste efektide erinevaid omadusi.<sup id="cite_ref-Negus_9-0" class="reference"><a href="#cite_note-Negus-9"><span class="cite-bracket">[</span>9<span class="cite-bracket">]</span></a></sup> Selle biokeemiline definitsiooni võtsid 1950. aastatel kasutusele <a href="/w/index.php?title=Ari%C3%ABns&action=edit&redlink=1" class="new" title="Ariëns (pole veel kirjutatud)">E. J. Ariëns</a><sup id="cite_ref-Ariëns_10-0" class="reference"><a href="#cite_note-Ariëns-10"><span class="cite-bracket">[</span>10<span class="cite-bracket">]</span></a></sup> ja <a href="/w/index.php?title=Mary_D._Stephenson&action=edit&redlink=1" class="new" title="Mary D. Stephenson (pole veel kirjutatud)">Mary D. Stephenson</a> <sup id="cite_ref-stephanson_11-0" class="reference"><a href="#cite_note-stephanson-11"><span class="cite-bracket">[</span>11<span class="cite-bracket">]</span></a></sup>. Praegune aktsepteeritud definitsioon põhineb <a href="/w/index.php?title=Retseptori_h%C3%B5ivatuse_mudel&action=edit&redlink=1" class="new" title="Retseptori hõivatuse mudel (pole veel kirjutatud)">retseptori hõivatuse mudelil</a>. See taandub antagonisti definitsioonile, mis arvestab ainult neid komponente, millel on vastupidised toimed ühele retseptorile. Aantagonistid lülitavad "sisse" <i>ühe</i> rakulise vastuse seondudes retseptorile, lükates käima biokeemilised protsessid, muutmaks rakku sisemiselt. Ning, et antagonistid lülitavad "välja" selle vastuse, blokeerides agonisti retseptorist. See definitsioon säilib samuti <a href="/w/index.php?title=F%C3%BCsioloogoline_antagonist&action=edit&redlink=1" class="new" title="Füsioloogoline antagonist (pole veel kirjutatud)">füsioloogilistes antagonistides</a> – ainetes, millel on vastupidised füsioloogilised omadused, kuid toimivad teistele retseptoritele. Nagu näiteks <a href="/wiki/Histamiin" title="Histamiin">histamiin</a> alandab vererõhku läbi <a href="/wiki/Vasodilatatsioon" title="Vasodilatatsioon">vasodilatatsiooni</a> histamiini H1 retseptoril, samal ajal kui <a href="/wiki/Adrenaliin" title="Adrenaliin">adrenaliin</a> tõstab arteriaalset rõhku läbi vasokontraktsiooni, mida vahendadakse läbi β-adrenergilise retseptori aktivatsiooniga. </p><p>Meie arusaam ravimi poolt indutseeritud mehhanismi aktivatsioonist ning biokeemilise definitsiooni retseptori antagonistist areneb tänaseni. Retseptori aktivatsiooni kahe-oleku mudel on andnud mitmeolekulisi mudeleid koos vahepealsete konformatsiooniliste olekutega.<sup id="cite_ref-Vauquelin_12-0" class="reference"><a href="#cite_note-Vauquelin-12"><span class="cite-bracket">[</span>12<span class="cite-bracket">]</span></a></sup> <a href="/w/index.php?title=Funktsionaalsuse_selektiivsuse&action=edit&redlink=1" class="new" title="Funktsionaalsuse selektiivsuse (pole veel kirjutatud)">Funktsionaalse selektiivsuse</a> avastamine ja et ligand-spetsiifilise retseptori konformatsioonide toimumine võib mõjutada teisi retseptoreid, millel on teistsugused signaalrajad, võib tähendada seda, et ravimeid saab disainida mingi kindla retseptori jaoks, kuid mitte ülejäänute jaoks. See omakorda tähendab seda, et tõhusus sõltub sellest, kus retseptor on ekspresseerunud, muutes me arusaamu, et retseptori efektiivsus on retseptorist mittesõltuv ravimi omadus<sup id="cite_ref-Urban2007_13-0" class="reference"><a href="#cite_note-Urban2007-13"><span class="cite-bracket">[</span>13<span class="cite-bracket">]</span></a></sup>. </p> <div class="mw-heading mw-heading2"><h2 id="Farmakodünaamika"><span id="Farmakod.C3.BCnaamika"></span>Farmakodünaamika</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=2" title="Muuda alaosa "Farmakodünaamika"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=2" title="Muuda alaosa "Farmakodünaamika" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <dl><dd><span typeof="mw:File"><span><img src="//upload.wikimedia.org/wikipedia/commons/thumb/a/a3/Next.svg/12px-Next.svg.png" decoding="async" width="12" height="12" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/a/a3/Next.svg/18px-Next.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/a/a3/Next.svg/24px-Next.svg.png 2x" data-file-width="160" data-file-height="160" /></span></span> <i>Pikemalt artiklis <a href="/w/index.php?title=Farmakod%C3%BCnaamika&action=edit&redlink=1" class="new" title="Farmakodünaamika (pole veel kirjutatud)">Farmakodünaamika</a></i></dd></dl> <div class="mw-heading mw-heading3"><h3 id="Efektiivsus_ja_potentsiaalsus">Efektiivsus ja potentsiaalsus</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=3" title="Muuda alaosa "Efektiivsus ja potentsiaalsus"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=3" title="Muuda alaosa "Efektiivsus ja potentsiaalsus" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>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 <a href="/w/index.php?title=Osaline_agonist&action=edit&redlink=1" class="new" title="Osaline agonist (pole veel kirjutatud)">osalise agonisti</a> funktsiooni. Funktsionaalsetes antagonistiproovides mõõdab <a href="/wiki/Doos-vastus_seos" class="mw-redirect" title="Doos-vastus seos">doos-vastus kurv</a> erinevatel kontsentratsioonidel antagonistide efekti võimet, kus nad suudavad pöörata ümber agonisti aktiivsust<sup id="cite_ref-2006Kenakin_4-2" class="reference"><a href="#cite_note-2006Kenakin-4"><span class="cite-bracket">[</span>4<span class="cite-bracket">]</span></a></sup>. Antagonisti potentsiaali mõõdetakse tema <a href="/wiki/IC50" title="IC50">IC<sub>50</sub></a> väärtusega. </p><p>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<sup id="cite_ref-Swinney2004_14-0" class="reference"><a href="#cite_note-Swinney2004-14"><span class="cite-bracket">[</span>14<span class="cite-bracket">]</span></a></sup>. </p> <div class="mw-heading mw-heading3"><h3 id="Afiinsus">Afiinsus</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=4" title="Muuda alaosa "Afiinsus"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=4" title="Muuda alaosa "Afiinsus" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Antagonisti ja <a href="/wiki/Seondumissait" title="Seondumissait">seondumissaidi</a> afiinsus (K<sub>i</sub>), </p><p><span class="mwe-math-element"><span class="mwe-math-mathml-inline mwe-math-mathml-a11y" style="display: none;"><math xmlns="http://www.w3.org/1998/Math/MathML" alttext="{\displaystyle K_{i}={\frac {IC_{50}}{1+{\frac {[S]}{K_{m}}}}}}"> <semantics> <mrow class="MJX-TeXAtom-ORD"> <mstyle displaystyle="true" scriptlevel="0"> <msub> <mi>K</mi> <mrow class="MJX-TeXAtom-ORD"> <mi>i</mi> </mrow> </msub> <mo>=</mo> <mrow class="MJX-TeXAtom-ORD"> <mfrac> <mrow> <mi>I</mi> <msub> <mi>C</mi> <mrow class="MJX-TeXAtom-ORD"> <mn>50</mn> </mrow> </msub> </mrow> <mrow> <mn>1</mn> <mo>+</mo> <mrow class="MJX-TeXAtom-ORD"> <mfrac> <mrow> <mo stretchy="false">[</mo> <mi>S</mi> <mo stretchy="false">]</mo> </mrow> <msub> <mi>K</mi> <mrow class="MJX-TeXAtom-ORD"> <mi>m</mi> </mrow> </msub> </mfrac> </mrow> </mrow> </mfrac> </mrow> </mstyle> </mrow> <annotation encoding="application/x-tex">{\displaystyle K_{i}={\frac {IC_{50}}{1+{\frac {[S]}{K_{m}}}}}}</annotation> </semantics> </math></span><img src="https://wikimedia.org/api/rest_v1/media/math/render/svg/d2446628b40cf387ddfaab015920ba224da669bd" class="mwe-math-fallback-image-inline mw-invert skin-invert" aria-hidden="true" style="vertical-align: -4.171ex; width:14.277ex; height:7.676ex;" alt="{\displaystyle K_{i}={\frac {IC_{50}}{1+{\frac {[S]}{K_{m}}}}}}"></span> </p><p>retseptori seostumise võime, määrab agonisti inhibeerimise aja. Antagonisti afiinsust võib määrata eksperimentaalselt, kasutades <a href="/w/index.php?title=Schildi_regressioon&action=edit&redlink=1" class="new" title="Schildi regressioon (pole veel kirjutatud)">Schildi regressiooni</a> või <a href="/w/index.php?title=Cheng-Prusoffi_v%C3%B5rrand&action=edit&redlink=1" class="new" title="Cheng-Prusoffi võrrand (pole veel kirjutatud)">Cheng-Prusoffi võrrandit</a> võistlevate antagonistide <a href="/w/index.php?title=Radioligand&action=edit&redlink=1" class="new" title="Radioligand (pole veel kirjutatud)">radioligandide</a> 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<sup id="cite_ref-Wyllie_15-0" class="reference"><a href="#cite_note-Wyllie-15"><span class="cite-bracket">[</span>15<span class="cite-bracket">]</span></a></sup><sup id="cite_ref-Colquhoun_16-0" class="reference"><a href="#cite_note-Colquhoun-16"><span class="cite-bracket">[</span>16<span class="cite-bracket">]</span></a></sup>. 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<sup id="cite_ref-Cheng_17-0" class="reference"><a href="#cite_note-Cheng-17"><span class="cite-bracket">[</span>17<span class="cite-bracket">]</span></a></sup>. Cheng-Prusoffi faktor võtab arvesse seda efekti, mis juhtub, kui muuta agonisti kontsentratsiooni ja afiinsust retseptoril, millel on juba võistlev inhibeeriv antagonist peal. </p> <div class="mw-heading mw-heading2"><h2 id="Tüübid"><span id="T.C3.BC.C3.BCbid"></span>Tüübid</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=5" title="Muuda alaosa "Tüübid"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=5" title="Muuda alaosa "Tüübid" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <div class="mw-heading mw-heading3"><h3 id="Võistlev"><span id="V.C3.B5istlev"></span>Võistlev</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=6" title="Muuda alaosa "Võistlev"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=6" title="Muuda alaosa "Võistlev" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <p><a href="/w/index.php?title=V%C3%B5istlev_antagonist&action=edit&redlink=1" class="new" title="Võistlev antagonist (pole veel kirjutatud)">Võistlevad antagonistid</a> (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<sup id="cite_ref-Swinney2004_14-1" class="reference"><a href="#cite_note-Swinney2004-14"><span class="cite-bracket">[</span>14<span class="cite-bracket">]</span></a></sup>. 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<sup id="cite_ref-Vauquelin2002_18-0" class="reference"><a href="#cite_note-Vauquelin2002-18"><span class="cite-bracket">[</span>18<span class="cite-bracket">]</span></a></sup>. </p><p><a href="/w/index.php?title=Interleukiin-1&action=edit&redlink=1" class="new" title="Interleukiin-1 (pole veel kirjutatud)">Interleukiin-1</a> retseptori antagonist IL-1Ra on üks näide võistlevast antagonistist<sup id="cite_ref-pmid8379462_19-0" class="reference"><a href="#cite_note-pmid8379462-19"><span class="cite-bracket">[</span>19<span class="cite-bracket">]</span></a></sup>. Võistleva antagonisti efekte võib alla suruda, tõstes agonisti kontsentratsiooni. Tihti (kuid mitte alati) omavad need antagonistid oma agonisti omaga väga sarnast keemilist struktuuri. </p> <div class="mw-heading mw-heading3"><h3 id="Mittevõistlev"><span id="Mittev.C3.B5istlev"></span>Mittevõistlev</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=7" title="Muuda alaosa "Mittevõistlev"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=7" title="Muuda alaosa "Mittevõistlev" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Terminit <i>mittevõistlev antagonist</i> (kutsutakse ka mitteületavaks antagonistiks) võidakse kasutada, et kirjeldada kaht omavahelist fenomeni: ühes, kus antagonist seondub retseptori seondumissaidile, teises, kus antagonist seob end <a href="/wiki/Allosteeriline" class="mw-redirect" title="Allosteeriline">allosteerilisele</a> saidile<sup id="cite_ref-Golan25_20-0" class="reference"><a href="#cite_note-Golan25-20"><span class="cite-bracket">[</span>20<span class="cite-bracket">]</span></a></sup>. Kuigi nende kahe fenomeni mehhanism on erinev, kutsutakse mõlemaid <i>mittevõistevaiks</i>, sellepärast et lõppetulemus on üpris sarnane. Erinevalt võistlevatest antagonistidest, mis mõjutavad agonisti taseme suurust, et saavutada maksimaalne vastus, kuid ei mõjuta maksimaalvastuse magnituudi, <i>mittevõitlevad agonistid</i> vähendavad selle maksimum-vastuse magnituudi, mille võib omandada ükskõik millise hulgaga agonist. See omadus teenib neile nime <i>mittevõistlev</i>, 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<sup id="cite_ref-Vauquelin2002_18-1" class="reference"><a href="#cite_note-Vauquelin2002-18"><span class="cite-bracket">[</span>18<span class="cite-bracket">]</span></a></sup>. Parempoolne kalle on retseptori reservi olemasolul ja agonisti vastuse inhibatsioon toimub ainult, kui reserv<sup id="cite_ref-stephanson_11-1" class="reference"><a href="#cite_note-stephanson-11"><span class="cite-bracket">[</span>11<span class="cite-bracket">]</span></a></sup> on ammendatud. </p><p>Antagonist, mis seob end retseptori aktiivsele saidile on <i>mittevõistlev</i> ainult siis, kui side aktiivsaidi ja antagonisti vahel on pöördumatu või sellele ligilähedane.<sup id="cite_ref-Golan25_20-1" class="reference"><a href="#cite_note-Golan25-20"><span class="cite-bracket">[</span>20<span class="cite-bracket">]</span></a></sup>. <i>Mittevõistleva</i> 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. </p><p><i>Mittevõistleva antagonisti</i> 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<sup id="cite_ref-Golan_21-0" class="reference"><a href="#cite_note-Golan-21"><span class="cite-bracket">[</span>21<span class="cite-bracket">]</span></a></sup>. </p> <div class="mw-heading mw-heading3"><h3 id="Konkurentsivõimetu"><span id="Konkurentsiv.C3.B5imetu"></span>Konkurentsivõimetu</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=8" title="Muuda alaosa "Konkurentsivõimetu"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=8" title="Muuda alaosa "Konkurentsivõimetu" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>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<sup id="cite_ref-Lipton_22-0" class="reference"><a href="#cite_note-Lipton-22"><span class="cite-bracket">[</span>22<span class="cite-bracket">]</span></a></sup>. Memantiin, mida kasutatakse <a href="/wiki/Alzheimeri_t%C3%B5bi" title="Alzheimeri tõbi">Alzheimeri tõve</a> ravimina, on samuti konkurentsivõimetu antagonist <a href="/w/index.php?title=NMDA_retseptor&action=edit&redlink=1" class="new" title="NMDA retseptor (pole veel kirjutatud)">NMDA retseptoril</a><sup id="cite_ref-Parsons_23-0" class="reference"><a href="#cite_note-Parsons-23"><span class="cite-bracket">[</span>23<span class="cite-bracket">]</span></a></sup>. </p> <div class="mw-heading mw-heading3"><h3 id="Vaikne_antagonist">Vaikne antagonist</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=9" title="Muuda alaosa "Vaikne antagonist"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=9" title="Muuda alaosa "Vaikne antagonist" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>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 <a href="/w/index.php?title=Osaline_antagonist&action=edit&redlink=1" class="new" title="Osaline antagonist (pole veel kirjutatud)">osalistest agonistidest</a> või <a href="/w/index.php?title=Inventeeritud_antagonist&action=edit&redlink=1" class="new" title="Inventeeritud antagonist (pole veel kirjutatud)">pöördagonistidest</a>. </p> <div class="mw-heading mw-heading2"><h2 id="Viited">Viited</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&veaction=edit&section=10" title="Muuda alaosa "Viited"" class="mw-editsection-visualeditor"><span>muuda</span></a><span class="mw-editsection-divider"> | </span><a href="/w/index.php?title=Antagonist_(farmakoloogia)&action=edit&section=10" title="Muuda alaosa "Viited" lähteteksti"><span>muuda lähteteksti</span></a><span class="mw-editsection-bracket">]</span></span></div> <div class="reflist" style="list-style-type: decimal;"> <div class="mw-references-wrap mw-references-columns"><ol class="references"> <li id="cite_note-pharmguide-1"><span class="mw-cite-backlink"><a href="#cite_ref-pharmguide_1-0">↑</a></span> <span class="reference-text">"<a rel="nofollow" class="external text" href="https://web.archive.org/web/20190726074523/http://www.pdg.cnb.uam.es/cursos/Barcelona2002/pages/Farmac/Comput_Lab/Guia_Glaxo/chap2c.html">Pharmacology Guide: In vitro pharmacology: concentration-response curves</a>." <i><a href="/wiki/GlaxoSmithKline" title="GlaxoSmithKline">GlaxoWellcome</a>.</i> Retrieved on December 6, 2007.</span> </li> <li id="cite_note-pmid12209152-2"><span class="mw-cite-backlink"><a href="#cite_ref-pmid12209152_2-0">↑</a></span> <span class="reference-text"><style data-mw-deduplicate="TemplateStyles:r6066747">.mw-parser-output cite.citation{font-style:inherit;word-wrap:break-word}.mw-parser-output .citation q{quotes:"\"""\"""'""'"}.mw-parser-output .citation:target{background-color:rgba(0,127,255,0.133)}.mw-parser-output .id-lock-free a,.mw-parser-output .citation .cs1-lock-free a{background:linear-gradient(transparent,transparent),url("//upload.wikimedia.org/wikipedia/commons/6/65/Lock-green.svg")right 0.1em center/9px no-repeat}.mw-parser-output .id-lock-limited a,.mw-parser-output .id-lock-registration a,.mw-parser-output .citation .cs1-lock-limited a,.mw-parser-output .citation .cs1-lock-registration a{background:linear-gradient(transparent,transparent),url("//upload.wikimedia.org/wikipedia/commons/d/d6/Lock-gray-alt-2.svg")right 0.1em center/9px no-repeat}.mw-parser-output .id-lock-subscription a,.mw-parser-output .citation .cs1-lock-subscription a{background:linear-gradient(transparent,transparent),url("//upload.wikimedia.org/wikipedia/commons/a/aa/Lock-red-alt-2.svg")right 0.1em center/9px no-repeat}.mw-parser-output .cs1-ws-icon a{background:linear-gradient(transparent,transparent),url("//upload.wikimedia.org/wikipedia/commons/4/4c/Wikisource-logo.svg")right 0.1em center/12px no-repeat}.mw-parser-output .cs1-code{color:inherit;background:inherit;border:none;padding:inherit}.mw-parser-output .cs1-hidden-error{display:none;color:#d33}.mw-parser-output .cs1-visible-error{color:#d33}.mw-parser-output .cs1-maint{display:none;color:#3a3;margin-left:0.3em}.mw-parser-output .cs1-format{font-size:95%}.mw-parser-output .cs1-kern-left{padding-left:0.2em}.mw-parser-output .cs1-kern-right{padding-right:0.2em}.mw-parser-output .citation .mw-selflink{font-weight:inherit}</style><cite id="CITEREFHopkins_AL,_Groom_CR2002" class="citation journal cs1">Hopkins AL, Groom CR (2002). 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"G protein-coupled receptors: a count of 1001 conformations". <i>Fundamental & clinical pharmacology</i>. <b>19</b> (1): 45–56.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Fundamental+%26+clinical+pharmacology&rft.atitle=G+protein-coupled+receptors%3A+a+count+of+1001+conformations&rft.volume=19&rft.issue=1&rft.pages=45-56&rft.date=2005&rft.au=Vauquelin+G%2C+Van+Liefde+I&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span></span> </li> <li id="cite_note-Urban2007-13"><span class="mw-cite-backlink"><a href="#cite_ref-Urban2007_13-0">↑</a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFUrban_JD,_Clarke_WP,_von_Zastrow_M2007" class="citation journal cs1">Urban JD, Clarke WP, von Zastrow M; et al. (2007). <a rel="nofollow" class="external text" href="https://archive.org/details/sim_journal-of-pharmacology-and-experimental-therapeutics_2007-01_320_1/page/1">"Functional selectivity and classical concepts of quantitative pharmacology"</a>. <i>J. Pharmacol. Exp. Ther</i>. <b>320</b> (1): 1–13.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=J.+Pharmacol.+Exp.+Ther.&rft.atitle=Functional+selectivity+and+classical+concepts+of+quantitative+pharmacology&rft.volume=320&rft.issue=1&rft.pages=1-13&rft.date=2007&rft.au=Urban+JD%2C+Clarke+WP%2C+von+Zastrow+M&rft_id=https%3A%2F%2Farchive.org%2Fdetails%2Fsim_journal-of-pharmacology-and-experimental-therapeutics_2007-01_320_1%2Fpage%2F1&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span> <span class="cs1-visible-error citation-comment"><code class="cs1-code">{{<a href="/wiki/Mall:Cite_journal" title="Mall:Cite journal">cite journal</a>}}</code>: </span><span class="cs1-visible-error citation-comment">et al.-i üleliigne kasutus kohas: <code class="cs1-code">|author=</code> (<a href="/wiki/Juhend:Viitamismallide_vead#explicit_et_al" title="Juhend:Viitamismallide vead">juhend</a>)</span><span class="cs1-maint citation-comment">CS1 hooldus: mitu nime: autorite loend (<a href="/wiki/Kategooria:CS1_hooldus:_mitu_nime:_autorite_loend" title="Kategooria:CS1 hooldus: mitu nime: autorite loend">link</a>)</span></span> </li> <li id="cite_note-Swinney2004-14"><span class="mw-cite-backlink">↑ <sup><a href="#cite_ref-Swinney2004_14-0">14,0</a></sup> <sup><a href="#cite_ref-Swinney2004_14-1">14,1</a></sup></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFSwinney_DC2004" class="citation journal cs1">Swinney DC (2004). "Biochemical mechanisms of drug action: what does it take for success?". <i>Nature reviews. Drug discovery</i>. <b>3</b> (9): 801–8.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Nature+reviews.+Drug+discovery&rft.atitle=Biochemical+mechanisms+of+drug+action%3A+what+does+it+take+for+success%3F&rft.volume=3&rft.issue=9&rft.pages=801-8&rft.date=2004&rft.au=Swinney+DC&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span></span> </li> <li id="cite_note-Wyllie-15"><span class="mw-cite-backlink"><a href="#cite_ref-Wyllie_15-0">↑</a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFWyllie_DJ,_Chen_PE2007" class="citation journal cs1">Wyllie DJ, Chen PE (2007). <a rel="nofollow" class="external text" href="https://archive.org/details/sim_british-journal-of-pharmacology_2007-03_150_5/page/541">"Taking the time to study competitive antagonism"</a>. <i>Br. J. Pharmacol</i>. <b>150</b> (5): 541–51.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Br.+J.+Pharmacol.&rft.atitle=Taking+the+time+to+study+competitive+antagonism&rft.volume=150&rft.issue=5&rft.pages=541-51&rft.date=2007&rft.au=Wyllie+DJ%2C+Chen+PE&rft_id=https%3A%2F%2Farchive.org%2Fdetails%2Fsim_british-journal-of-pharmacology_2007-03_150_5%2Fpage%2F541&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span></span> </li> <li id="cite_note-Colquhoun-16"><span class="mw-cite-backlink"><a href="#cite_ref-Colquhoun_16-0">↑</a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFColquhoun_D2007" class="citation journal cs1">Colquhoun D (2007). "Why the Schild method is better than Schild realised". <i>Trends Pharmacol Sci</i>. <b>28</b> (12): 608.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Trends+Pharmacol+Sci&rft.atitle=Why+the+Schild+method+is+better+than+Schild+realised&rft.volume=28&rft.issue=12&rft.pages=608&rft.date=2007&rft.au=Colquhoun+D&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span></span> </li> <li id="cite_note-Cheng-17"><span class="mw-cite-backlink"><a href="#cite_ref-Cheng_17-0">↑</a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFCheng_Y,_Prusoff_WH1973" class="citation journal cs1">Cheng Y, Prusoff WH (1973). "Relationship between the inhibition constant (K1) and the concentration of inhibitor, which causes 50 per cent inhibition (I50) of an enzymatic reaction". <i>Biochem. Pharmacol</i>. <b>22</b> (23): 3099–108.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Biochem.+Pharmacol.&rft.atitle=Relationship+between+the+inhibition+constant+%28K1%29+and+the+concentration+of+inhibitor%2C+which+causes+50+per+cent+inhibition+%28I50%29+of+an+enzymatic+reaction&rft.volume=22&rft.issue=23&rft.pages=3099-108&rft.date=1973&rft.au=Cheng+Y%2C+Prusoff+WH&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span></span> </li> <li id="cite_note-Vauquelin2002-18"><span class="mw-cite-backlink">↑ <sup><a href="#cite_ref-Vauquelin2002_18-0">18,0</a></sup> <sup><a href="#cite_ref-Vauquelin2002_18-1">18,1</a></sup></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFVauquelin_G,_Van_Liefde_I,_Birzbier_BB,_Vanderheyden_PM2002" class="citation journal cs1">Vauquelin G, Van Liefde I, Birzbier BB, Vanderheyden PM (2002). "New insights in insurmountable antagonism". <i>Fundamental & clinical pharmacology</i>. <b>16</b> (4): 263–72.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Fundamental+%26+clinical+pharmacology&rft.atitle=New+insights+in+insurmountable+antagonism&rft.volume=16&rft.issue=4&rft.pages=263-72&rft.date=2002&rft.au=Vauquelin+G%2C+Van+Liefde+I%2C+Birzbier+BB%2C+Vanderheyden+PM&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span><span class="cs1-maint citation-comment"><code class="cs1-code">{{<a href="/wiki/Mall:Cite_journal" title="Mall:Cite journal">cite journal</a>}}</code>: CS1 hooldus: mitu nime: autorite loend (<a href="/wiki/Kategooria:CS1_hooldus:_mitu_nime:_autorite_loend" title="Kategooria:CS1 hooldus: mitu nime: autorite loend">link</a>)</span></span> </li> <li id="cite_note-pmid8379462-19"><span class="mw-cite-backlink"><a href="#cite_ref-pmid8379462_19-0">↑</a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFArend_WP1993" class="citation journal cs1">Arend WP (1993). "Interleukin-1 receptor antagonist". <i>Adv. Immunol</i>. <b>54</b>: 167–227.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Adv.+Immunol.&rft.atitle=Interleukin-1+receptor+antagonist&rft.volume=54&rft.pages=167-227&rft.date=1993&rft.au=Arend+WP&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span></span> </li> <li id="cite_note-Golan25-20"><span class="mw-cite-backlink">↑ <sup><a href="#cite_ref-Golan25_20-0">20,0</a></sup> <sup><a href="#cite_ref-Golan25_20-1">20,1</a></sup></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFeds2008" class="citation book cs1">eds, David E. Golan, ed.-in-chief ; Armen H. Tashjian, Jr., deputy ed. ; Ehrin J. Armstrong, April W. Armstrong, associate (2008). <a rel="nofollow" class="external text" href="http://books.google.com/books?id=az8uSDkB0mgC&pg=PA23&lpg=PA23&dq=noncompetitive+active+site+antagonist#v=onepage&q&f=false"><i>Principles of pharmacology : the pathophysiologic basis of drug therapy</i></a> (2nd ed. ed.). Philadelphia, Pa., [etc.]: Lippincott Williams & Wilkins. Lk 25. <a href="/wiki/Rahvusvaheline_raamatu_standardnumber" title="Rahvusvaheline raamatu standardnumber">ISBN</a> <a href="/wiki/Eri:Raamatuotsimine/9780781783552" title="Eri:Raamatuotsimine/9780781783552"><bdi>9780781783552</bdi></a>.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Abook&rft.genre=book&rft.btitle=Principles+of+pharmacology+%3A+the+pathophysiologic+basis+of+drug+therapy&rft.place=Philadelphia%2C+Pa.%2C+%5Betc.%5D&rft.pages=25&rft.edition=2nd+ed.&rft.pub=Lippincott+Williams+%26+Wilkins&rft.date=2008&rft.isbn=9780781783552&rft.aulast=eds&rft.aufirst=David+E.+Golan%2C+ed.-in-chief+%3B+Armen+H.+Tashjian%2C+Jr.%2C+deputy+ed.+%3B+Ehrin+J.+Armstrong%2C+April+W.+Armstrong%2C+associate&rft_id=http%3A%2F%2Fbooks.google.com%2Fbooks%3Fid%3Daz8uSDkB0mgC%26pg%3DPA23%26lpg%3DPA23%26dq%3Dnoncompetitive%2Bactive%2Bsite%2Bantagonist%23v%3Donepage%26q%26f%3Dfalse&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span> <span class="cs1-visible-error citation-comment"><code class="cs1-code">{{<a href="/wiki/Mall:Cite_book" title="Mall:Cite book">cite book</a>}}</code>: </span><span class="cs1-visible-error citation-comment">parameetris <code class="cs1-code">|edition=</code> on üleliigne tekst (<a href="/wiki/Juhend:Viitamismallide_vead#extra_text_edition" title="Juhend:Viitamismallide vead">juhend</a>)</span></span> </li> <li id="cite_note-Golan-21"><span class="mw-cite-backlink"><a href="#cite_ref-Golan_21-0">↑</a></span> <span class="reference-text">D.E. Golan, A.H Tashjian Jr, E.J. Armstrong, A.W. Armstrong. (2007) Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy Lippincott Williams & Wilkins <a href="/wiki/Eri:Raamatuotsimine/0781783550" class="internal mw-magiclink-isbn">ISBN 0-7817-8355-0</a></span> </li> <li id="cite_note-Lipton-22"><span class="mw-cite-backlink"><a href="#cite_ref-Lipton_22-0">↑</a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFLipton_SA2004" class="citation journal cs1">Lipton SA (2004). "Failures and successes of NMDA receptor antagonists: molecular basis for the use of open-channel blockers like memantine in the treatment of acute and chronic neurologic insults". <i>NeuroRx : the journal of the American Society for Experimental NeuroTherapeutics</i>. <b>1</b> (1): 101–10.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=NeuroRx+%3A+the+journal+of+the+American+Society+for+Experimental+NeuroTherapeutics&rft.atitle=Failures+and+successes+of+NMDA+receptor+antagonists%3A+molecular+basis+for+the+use+of+open-channel+blockers+like+memantine+in+the+treatment+of+acute+and+chronic+neurologic+insults&rft.volume=1&rft.issue=1&rft.pages=101-10&rft.date=2004&rft.au=Lipton+SA&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span></span> </li> <li id="cite_note-Parsons-23"><span class="mw-cite-backlink"><a href="#cite_ref-Parsons_23-0">↑</a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r6066747"><cite id="CITEREFParsons_CG,_Stöffler_A,_Danysz_W2007" class="citation journal cs1">Parsons CG, Stöffler A, Danysz W (2007). "Memantine: a NMDA receptor antagonist that improves memory by restoration of homeostasis in the glutamatergic system – too little activation is bad, too much is even worse". <i>Neuropharmacology</i>. <b>53</b> (6): 699–723.</cite><span title="ctx_ver=Z39.88-2004&rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&rft.genre=article&rft.jtitle=Neuropharmacology&rft.atitle=Memantine%3A+a+NMDA+receptor+antagonist+that+improves+memory+by+restoration+of+homeostasis+in+the+glutamatergic+system+%E2%80%93+too+little+activation+is+bad%2C+too+much+is+even+worse&rft.volume=53&rft.issue=6&rft.pages=699-723&rft.date=2007&rft.au=Parsons+CG%2C+St%C3%B6ffler+A%2C+Danysz+W&rfr_id=info%3Asid%2Fet.wikipedia.org%3AAntagonist+%28farmakoloogia%29" class="Z3988"></span><span class="cs1-maint citation-comment"><code class="cs1-code">{{<a href="/wiki/Mall:Cite_journal" title="Mall:Cite journal">cite journal</a>}}</code>: CS1 hooldus: mitu nime: autorite loend (<a href="/wiki/Kategooria:CS1_hooldus:_mitu_nime:_autorite_loend" title="Kategooria:CS1 hooldus: mitu nime: autorite loend">link</a>)</span></span> </li> </ol></div></div>    </div><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/w/index.php?title=Antagonist_(farmakoloogia)&oldid=6714489">https://et.wikipedia.org/w/index.php?title=Antagonist_(farmakoloogia)&oldid=6714489</a>"</div></div> <div id="catlinks" class="catlinks" data-mw="interface"><div id="mw-normal-catlinks" class="mw-normal-catlinks"><a href="/wiki/Eri:Kategooriad" title="Eri:Kategooriad">Kategooria</a>: <ul><li><a href="/wiki/Kategooria:Farmakoloogia" title="Kategooria:Farmakoloogia">Farmakoloogia</a></li></ul></div><div id="mw-hidden-catlinks" class="mw-hidden-catlinks mw-hidden-cats-hidden">Peidetud kategooriad: <ul><li><a href="/wiki/Kategooria:CS1_hooldus:_mitu_nime:_autorite_loend" title="Kategooria:CS1 hooldus: mitu nime: autorite loend">CS1 hooldus: mitu nime: autorite loend</a></li><li><a href="/wiki/Kategooria:CS1_vead:_et_al." title="Kategooria:CS1 vead: et al.">CS1 vead: et al.</a></li><li><a href="/wiki/Kategooria:CS1_vead:_%C3%BCleliigne_tekst:_tr%C3%BCkk" title="Kategooria:CS1 vead: üleliigne tekst: trükk">CS1 vead: üleliigne tekst: trükk</a></li><li><a href="/wiki/Kategooria:ISBN-v%C3%B5lulingiga_lehek%C3%BCljed" title="Kategooria:ISBN-võlulingiga leheküljed">ISBN-võlulingiga leheküljed</a></li><li><a href="/wiki/Kategooria:Toimetamist_ootavad_(jaanuar_2012)" title="Kategooria:Toimetamist ootavad (jaanuar 2012)">Toimetamist ootavad (jaanuar 2012)</a></li><li><a href="/wiki/Kategooria:Toimetamist_ootavad" title="Kategooria:Toimetamist ootavad">Toimetamist ootavad</a></li></ul></div></div> </div> </main> </div> <div class="mw-footer-container"> <footer id="footer" class="mw-footer" > <ul id="footer-info"> <li id="footer-info-lastmod"> Selle lehekülje viimane muutmine: 12:01, 27. august 2024.</li> <li id="footer-info-copyright">Tekst on kasutatav vastavalt Creative Commonsi litsentsile "<a rel="nofollow" class="external text" href="https://creativecommons.org/licenses/by-sa/4.0/deed.et">Autorile viitamine + jagamine samadel tingimustel</a>"; sellele võivad lisanduda täiendavad tingimused. 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