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Agonist - Wikipedia

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</button> <ul id="toc-Activity-sublist" class="vector-toc-list"> <li id="toc-Potency" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Potency"> <div class="vector-toc-text"> <span class="vector-toc-numb">4.1</span> <span>Potency</span> </div> </a> <ul id="toc-Potency-sublist" class="vector-toc-list"> </ul> </li> <li id="toc-Therapeutic_index" class="vector-toc-list-item vector-toc-level-2"> <a class="vector-toc-link" href="#Therapeutic_index"> <div class="vector-toc-text"> <span class="vector-toc-numb">4.2</span> <span>Therapeutic index</span> </div> </a> <ul id="toc-Therapeutic_index-sublist" class="vector-toc-list"> </ul> </li> </ul> </li> <li id="toc-See_also" class="vector-toc-list-item vector-toc-level-1 vector-toc-list-item-expanded"> <a class="vector-toc-link" href="#See_also"> <div class="vector-toc-text"> <span class="vector-toc-numb">5</span> <span>See also</span> </div> </a> <ul id="toc-See_also-sublist" class="vector-toc-list"> </ul> </li> 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Available in 35 languages" > <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-35" 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">35 languages</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%86%D8%A7%D9%87%D8%B6_(%D8%B9%D9%84%D9%85_%D8%A7%D9%84%D8%A3%D8%AF%D9%88%D9%8A%D8%A9)" title="ناهض (علم الأدوية) – Arabic" lang="ar" hreflang="ar" data-title="ناهض (علم الأدوية)" data-language-autonym="العربية" data-language-local-name="Arabic" class="interlanguage-link-target"><span>العربية</span></a></li><li class="interlanguage-link interwiki-bn mw-list-item"><a href="https://bn.wikipedia.org/wiki/%E0%A6%95%E0%A7%8D%E0%A6%B0%E0%A6%BF%E0%A6%AF%E0%A6%BC%E0%A6%9C_%E0%A6%AA%E0%A6%A6%E0%A6%BE%E0%A6%B0%E0%A7%8D%E0%A6%A5" title="ক্রিয়জ পদার্থ – Bangla" lang="bn" hreflang="bn" data-title="ক্রিয়জ পদার্থ" data-language-autonym="বাংলা" data-language-local-name="Bangla" class="interlanguage-link-target"><span>বাংলা</span></a></li><li class="interlanguage-link interwiki-ca mw-list-item"><a href="https://ca.wikipedia.org/wiki/Agonista" title="Agonista – Catalan" lang="ca" hreflang="ca" data-title="Agonista" data-language-autonym="Català" data-language-local-name="Catalan" class="interlanguage-link-target"><span>Català</span></a></li><li class="interlanguage-link interwiki-da mw-list-item"><a href="https://da.wikipedia.org/wiki/Agonist_(farmakologi)" title="Agonist (farmakologi) – Danish" lang="da" hreflang="da" data-title="Agonist (farmakologi)" data-language-autonym="Dansk" data-language-local-name="Danish" class="interlanguage-link-target"><span>Dansk</span></a></li><li class="interlanguage-link interwiki-de mw-list-item"><a href="https://de.wikipedia.org/wiki/Agonist_(Pharmakologie)" title="Agonist (Pharmakologie) – German" lang="de" hreflang="de" data-title="Agonist (Pharmakologie)" data-language-autonym="Deutsch" data-language-local-name="German" class="interlanguage-link-target"><span>Deutsch</span></a></li><li class="interlanguage-link interwiki-et mw-list-item"><a href="https://et.wikipedia.org/wiki/Agonist" title="Agonist – Estonian" lang="et" hreflang="et" data-title="Agonist" data-language-autonym="Eesti" data-language-local-name="Estonian" class="interlanguage-link-target"><span>Eesti</span></a></li><li class="interlanguage-link interwiki-es mw-list-item"><a href="https://es.wikipedia.org/wiki/Agonista" title="Agonista – Spanish" lang="es" hreflang="es" data-title="Agonista" data-language-autonym="Español" data-language-local-name="Spanish" 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/Agonista" title="Agonista – Basque" lang="eu" hreflang="eu" data-title="Agonista" data-language-autonym="Euskara" data-language-local-name="Basque" 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%DA%AF%D9%88%D9%86%DB%8C%D8%B3%D8%AA" title="آگونیست – Persian" lang="fa" hreflang="fa" data-title="آگونیست" data-language-autonym="فارسی" data-language-local-name="Persian" 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/Agoniste_(biochimie)" title="Agoniste (biochimie) – French" lang="fr" hreflang="fr" data-title="Agoniste (biochimie)" data-language-autonym="Français" data-language-local-name="French" 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/%ED%9A%A8%EB%8A%A5%EC%A0%9C" title="효능제 – Korean" lang="ko" hreflang="ko" data-title="효능제" data-language-autonym="한국어" data-language-local-name="Korean" 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/Agonist_(kemija)" title="Agonist (kemija) – Croatian" lang="hr" hreflang="hr" data-title="Agonist (kemija)" data-language-autonym="Hrvatski" data-language-local-name="Croatian" 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%B0taka%C3%B6rvi" title="Viðtakaörvi – Icelandic" lang="is" hreflang="is" data-title="Viðtakaörvi" data-language-autonym="Íslenska" data-language-local-name="Icelandic" 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/Agonista" title="Agonista – Italian" lang="it" hreflang="it" data-title="Agonista" data-language-autonym="Italiano" data-language-local-name="Italian" 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%92%D7%95%D7%A0%D7%99%D7%A1%D7%98" title="אגוניסט – Hebrew" lang="he" hreflang="he" data-title="אגוניסט" data-language-autonym="עברית" data-language-local-name="Hebrew" class="interlanguage-link-target"><span>עברית</span></a></li><li class="interlanguage-link interwiki-la mw-list-item"><a href="https://la.wikipedia.org/wiki/Agonista_(biochemia)" title="Agonista (biochemia) – Latin" lang="la" hreflang="la" data-title="Agonista (biochemia)" data-language-autonym="Latina" data-language-local-name="Latin" class="interlanguage-link-target"><span>Latina</span></a></li><li class="interlanguage-link interwiki-hu mw-list-item"><a href="https://hu.wikipedia.org/wiki/Agonista" title="Agonista – Hungarian" lang="hu" hreflang="hu" data-title="Agonista" data-language-autonym="Magyar" data-language-local-name="Hungarian" class="interlanguage-link-target"><span>Magyar</span></a></li><li class="interlanguage-link interwiki-nl mw-list-item"><a href="https://nl.wikipedia.org/wiki/Agonist_(biochemie)" title="Agonist (biochemie) – Dutch" lang="nl" hreflang="nl" data-title="Agonist (biochemie)" data-language-autonym="Nederlands" data-language-local-name="Dutch" 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/%E3%82%A2%E3%82%B4%E3%83%8B%E3%82%B9%E3%83%88" title="アゴニスト – Japanese" lang="ja" hreflang="ja" data-title="アゴニスト" data-language-autonym="日本語" data-language-local-name="Japanese" class="interlanguage-link-target"><span>日本語</span></a></li><li class="interlanguage-link interwiki-no mw-list-item"><a href="https://no.wikipedia.org/wiki/Agonist" title="Agonist – Norwegian Bokmål" lang="nb" hreflang="nb" data-title="Agonist" data-language-autonym="Norsk bokmål" data-language-local-name="Norwegian Bokmål" class="interlanguage-link-target"><span>Norsk bokmål</span></a></li><li class="interlanguage-link interwiki-pl mw-list-item"><a href="https://pl.wikipedia.org/wiki/Agonista" title="Agonista – Polish" lang="pl" hreflang="pl" data-title="Agonista" data-language-autonym="Polski" data-language-local-name="Polish" 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/Agonista_(farmacologia)" title="Agonista (farmacologia) – Portuguese" lang="pt" hreflang="pt" data-title="Agonista (farmacologia)" data-language-autonym="Português" data-language-local-name="Portuguese" 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/Agonist" title="Agonist – Romanian" lang="ro" hreflang="ro" data-title="Agonist" data-language-autonym="Română" data-language-local-name="Romanian" 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%B3%D0%BE%D0%BD%D0%B8%D1%81%D1%82" title="Агонист – Russian" lang="ru" hreflang="ru" data-title="Агонист" data-language-autonym="Русский" data-language-local-name="Russian" 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/Agonist" title="Agonist – Simple English" lang="en-simple" hreflang="en-simple" data-title="Agonist" data-language-autonym="Simple English" data-language-local-name="Simple English" 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/Agonist" title="Agonist – Slovenian" lang="sl" hreflang="sl" data-title="Agonist" data-language-autonym="Slovenščina" data-language-local-name="Slovenian" class="interlanguage-link-target"><span>Slovenščina</span></a></li><li class="interlanguage-link interwiki-ckb mw-list-item"><a href="https://ckb.wikipedia.org/wiki/%D8%A6%D8%A7%DA%AF%DB%86%D9%86%DB%8C%D8%B3%D8%AA" title="ئاگۆنیست – Central Kurdish" lang="ckb" hreflang="ckb" data-title="ئاگۆنیست" data-language-autonym="کوردی" data-language-local-name="Central Kurdish" class="interlanguage-link-target"><span>کوردی</span></a></li><li class="interlanguage-link interwiki-sr mw-list-item"><a href="https://sr.wikipedia.org/wiki/Agonist_(farmakologija)" title="Agonist (farmakologija) – Serbian" lang="sr" hreflang="sr" data-title="Agonist (farmakologija)" data-language-autonym="Српски / srpski" data-language-local-name="Serbian" 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/Agonist_(farmakologija)" title="Agonist (farmakologija) – Serbo-Croatian" lang="sh" hreflang="sh" data-title="Agonist (farmakologija)" data-language-autonym="Srpskohrvatski / српскохрватски" data-language-local-name="Serbo-Croatian" 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/Agonisti" title="Agonisti – Finnish" lang="fi" hreflang="fi" data-title="Agonisti" data-language-autonym="Suomi" data-language-local-name="Finnish" 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/Agonist" title="Agonist – Swedish" lang="sv" hreflang="sv" data-title="Agonist" data-language-autonym="Svenska" data-language-local-name="Swedish" 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%B8%95%E0%B8%B1%E0%B8%A7%E0%B8%97%E0%B8%B3%E0%B8%81%E0%B8%B2%E0%B8%A3" title="ตัวทำการ – Thai" lang="th" hreflang="th" data-title="ตัวทำการ" data-language-autonym="ไทย" data-language-local-name="Thai" class="interlanguage-link-target"><span>ไทย</span></a></li><li class="interlanguage-link interwiki-tr mw-list-item"><a href="https://tr.wikipedia.org/wiki/Agonist" title="Agonist – Turkish" lang="tr" hreflang="tr" data-title="Agonist" data-language-autonym="Türkçe" data-language-local-name="Turkish" class="interlanguage-link-target"><span>Türkçe</span></a></li><li class="interlanguage-link interwiki-uk mw-list-item"><a href="https://uk.wikipedia.org/wiki/%D0%90%D0%B3%D0%BE%D0%BD%D1%96%D1%81%D1%82" title="Агоніст – Ukrainian" lang="uk" hreflang="uk" data-title="Агоніст" data-language-autonym="Українська" data-language-local-name="Ukrainian" class="interlanguage-link-target"><span>Українська</span></a></li><li class="interlanguage-link interwiki-zh mw-list-item"><a href="https://zh.wikipedia.org/wiki/%E6%BF%80%E5%8A%A8%E5%89%82" title="激动剂 – Chinese" lang="zh" hreflang="zh" data-title="激动剂" data-language-autonym="中文" data-language-local-name="Chinese" class="interlanguage-link-target"><span>中文</span></a></li> </ul> <div class="after-portlet after-portlet-lang"><span class="wb-langlinks-edit wb-langlinks-link"><a href="https://www.wikidata.org/wiki/Special:EntityPage/Q389934#sitelinks-wikipedia" title="Edit interlanguage links" class="wbc-editpage">Edit links</a></span></div> </div> </div> </div> </header> <div class="vector-page-toolbar"> <div class="vector-page-toolbar-container"> <div id="left-navigation"> <nav aria-label="Namespaces"> <div id="p-associated-pages" class="vector-menu 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print{body.ns-0 .mw-parser-output .hatnote{display:none!important}}</style><div role="note" class="hatnote navigation-not-searchable"><span>For other uses of "Agonist" or "Agonism", see <a href="/wiki/Agonist_(disambiguation)" class="mw-disambig" title="Agonist (disambiguation)">Agonist (disambiguation)</a>.</span> <span>For a primary fictional character in a work, see <a href="/wiki/Protagonist" title="Protagonist">Protagonist</a> and <a href="/wiki/Antagonist" title="Antagonist">Antagonist</a>.</span></div> <figure typeof="mw:File/Thumb"><a href="/wiki/File:Inverse_agonist_3.svg" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/6/6c/Inverse_agonist_3.svg/400px-Inverse_agonist_3.svg.png" decoding="async" width="400" height="219" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/6/6c/Inverse_agonist_3.svg/600px-Inverse_agonist_3.svg.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/6/6c/Inverse_agonist_3.svg/800px-Inverse_agonist_3.svg.png 2x" data-file-width="534" data-file-height="293" /></a><figcaption>Dose response curves of a full agonist, partial agonist, neutral antagonist, and inverse agonist</figcaption></figure> <p>An <b>agonist</b> is a chemical that activates a <a href="/wiki/Receptor_(biochemistry)" title="Receptor (biochemistry)">receptor</a> to produce a biological response. Receptors are <a href="/wiki/Cell_(biology)" title="Cell (biology)">cellular</a> <a href="/wiki/Proteins" class="mw-redirect" title="Proteins">proteins</a> whose activation causes the cell to modify what it is currently doing. In contrast, an <a href="/wiki/Receptor_antagonist" title="Receptor antagonist">antagonist</a> blocks the action of the agonist, while an <a href="/wiki/Inverse_agonist" title="Inverse agonist">inverse agonist</a> causes an action opposite to that of the agonist. </p> <meta property="mw:PageProp/toc" /> <div class="mw-heading mw-heading2"><h2 id="Etymology">Etymology</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=1" title="Edit section: Etymology"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>From the <a href="/wiki/Ancient_Greek_language" class="mw-redirect" title="Ancient Greek language">Greek</a> <b>αγωνιστής</b> (agōnistēs), contestant; champion; rival &lt; <b>αγων</b> (agōn), contest, combat; exertion, struggle &lt; <b>αγω</b> (agō), I lead, lead towards, conduct; drive </p> <div class="mw-heading mw-heading2"><h2 id="Types_of_agonists"><span class="anchor" id="Full_agonist"></span><span class="anchor" id="Types"></span>Types of agonists</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=2" title="Edit section: Types of agonists"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p><a href="/wiki/Receptor_(biochemistry)" title="Receptor (biochemistry)">Receptors</a> can be activated by either <a href="/wiki/Endogenous" class="mw-redirect" title="Endogenous">endogenous</a> agonists (such as <a href="/wiki/Hormone" title="Hormone">hormones</a> and <a href="/wiki/Neurotransmitter" title="Neurotransmitter">neurotransmitters</a>) or <a href="/wiki/Exogenous" class="mw-redirect" title="Exogenous">exogenous</a> agonists (such as <a href="/wiki/Medication" title="Medication">drugs</a>), resulting in a biological response. A <a href="/wiki/Physiological_agonism_and_antagonism" title="Physiological agonism and antagonism">physiological agonist</a> is a substance that creates the same bodily responses but does not bind to the same receptor. </p> <ul><li>An <a href="/wiki/Endogenous_agonist" title="Endogenous agonist">endogenous agonist</a> for a particular receptor is a compound naturally produced by the body that binds to and activates that receptor. For example, the endogenous agonist for <a href="/wiki/5-HT_receptor" title="5-HT receptor">serotonin receptors</a> is <a href="/wiki/Serotonin" title="Serotonin">serotonin</a>, and the endogenous agonist for <a href="/wiki/Dopamine_receptor" title="Dopamine receptor">dopamine receptors</a> is <a href="/wiki/Dopamine" title="Dopamine">dopamine</a>.<sup id="cite_ref-1" class="reference"><a href="#cite_note-1"><span class="cite-bracket">&#91;</span>1<span class="cite-bracket">&#93;</span></a></sup></li> <li><b>Full agonists</b> bind to and activate a receptor with the maximum response that an agonist can elicit at the receptor. One example of a drug that can act as a full agonist is <a href="/wiki/Isoproterenol" class="mw-redirect" title="Isoproterenol">isoproterenol</a>, which mimics the action of <a href="/wiki/Epinephrine" class="mw-redirect" title="Epinephrine">adrenaline</a> at <a href="/wiki/Adrenergic_receptor" title="Adrenergic receptor">β adrenoreceptors</a>. Another example is <a href="/wiki/Morphine" title="Morphine">morphine</a>, which mimics the actions of <a href="/wiki/Endorphin" class="mw-redirect" title="Endorphin">endorphins</a> at <a href="/wiki/%CE%9C-opioid_receptor" title="Μ-opioid receptor">μ-opioid receptors</a> throughout the <a href="/wiki/Central_nervous_system" title="Central nervous system">central nervous system</a>. However, a drug can act as a full agonist in some tissues and as a partial agonist in other tissues, depending upon the relative numbers of receptors and differences in receptor coupling.<sup class="noprint Inline-Template Template-Fact" style="white-space:nowrap;">&#91;<i><a href="/wiki/Wikipedia:Identifying_reliable_sources_(medicine)" title="Wikipedia:Identifying reliable sources (medicine)"><span title="Material near this tag needs references to reliable medical sources. (December 2017)">medical citation needed</span></a></i>&#93;</sup></li> <li>A <b>co-agonist</b> works with other co-agonists to produce the desired effect together. <a href="/wiki/NMDA_receptor" title="NMDA receptor">NMDA receptor</a> activation requires the binding of both <a href="/wiki/Glutamate" class="mw-redirect" title="Glutamate">glutamate</a>, <a href="/wiki/Glycine" title="Glycine">glycine</a> and D-serine co-agonists. <a href="/wiki/Calcium_in_biology" title="Calcium in biology">Calcium</a> can also act as a co-agonist at the <a href="/wiki/IP3_receptor" class="mw-redirect" title="IP3 receptor">IP3 receptor</a>.</li> <li>A <b>selective agonist</b> is selective for a specific type of receptor. E.g. <a href="/wiki/Buspirone" title="Buspirone">buspirone</a> is a selective agonist for serotonin 5-HT1A.</li> <li><a href="/wiki/Partial_agonist" title="Partial agonist">Partial agonists</a> (such as <a href="/wiki/Buspirone" title="Buspirone">buspirone</a>, <a href="/wiki/Aripiprazole" title="Aripiprazole">aripiprazole</a>, <a href="/wiki/Buprenorphine" title="Buprenorphine">buprenorphine</a>, or <a href="/wiki/Clozapine" title="Clozapine">norclozapine</a>) also bind and activate a given receptor, but have only partial <a href="/wiki/Intrinsic_activity" title="Intrinsic activity">efficacy</a> at the receptor relative to a full agonist, even at maximal receptor occupancy. Agents like <a href="/wiki/Buprenorphine" title="Buprenorphine">buprenorphine</a> are used to treat <a href="/wiki/Opiate" title="Opiate">opiate</a> dependence for this reason, as they produce milder effects on the opioid receptor with lower dependence and abuse potential.</li> <li>An <a href="/wiki/Inverse_agonist" title="Inverse agonist">inverse agonist</a> is an agent that binds to the same receptor binding-site as an agonist for that receptor and inhibits the constitutive activity of the receptor. <a href="/wiki/Inverse_agonist" title="Inverse agonist">Inverse agonists</a> exert the opposite pharmacological effect of a receptor agonist, not merely an absence of the agonist effect as seen with an <a href="/wiki/Receptor_antagonist" title="Receptor antagonist">antagonist</a>. An example is the cannabinoid inverse agonist <a href="/wiki/Rimonabant" title="Rimonabant">rimonabant</a>.</li> <li>A <a href="/wiki/Superagonist" title="Superagonist">superagonist</a> is a term used by some to identify a compound that is capable of producing a greater response than the <a href="/wiki/Endogenous_agonist" title="Endogenous agonist">endogenous agonist</a> for the target receptor. It might be argued that the endogenous agonist is simply a partial agonist in that tissue.</li> <li>An <a href="/wiki/Irreversible_agonist" title="Irreversible agonist">irreversible agonist</a> is a type of agonist that binds permanently to a receptor through the formation of covalent bonds.<sup id="cite_ref-2" class="reference"><a href="#cite_note-2"><span class="cite-bracket">&#91;</span>2<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-3" class="reference"><a href="#cite_note-3"><span class="cite-bracket">&#91;</span>3<span class="cite-bracket">&#93;</span></a></sup></li> <li>A <a href="/wiki/Functional_selectivity" title="Functional selectivity">biased agonist</a> is an agent that binds to a receptor without affecting the same signal transduction pathway. <a href="/wiki/Oliceridine" title="Oliceridine">Oliceridine</a> is a μ-opioid receptor agonist that has been described to be functionally selective towards G protein and away from β-arrestin2 pathways.<sup id="cite_ref-pmid23300227_4-0" class="reference"><a href="#cite_note-pmid23300227-4"><span class="cite-bracket">&#91;</span>4<span class="cite-bracket">&#93;</span></a></sup></li></ul> <p>New findings that broaden the conventional definition of pharmacology demonstrate that <a href="/wiki/Ligand_(biochemistry)" title="Ligand (biochemistry)">ligands</a> can concurrently behave as agonist <i>and</i> antagonists at the same receptor, depending on effector pathways or tissue type. Terms that describe this phenomenon are "<a href="/wiki/Functional_selectivity" title="Functional selectivity">functional selectivity</a>", "protean agonism",<sup id="cite_ref-pmid11259378_5-0" class="reference"><a href="#cite_note-pmid11259378-5"><span class="cite-bracket">&#91;</span>5<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-pmid16803859_6-0" class="reference"><a href="#cite_note-pmid16803859-6"><span class="cite-bracket">&#91;</span>6<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-7" class="reference"><a href="#cite_note-7"><span class="cite-bracket">&#91;</span>7<span class="cite-bracket">&#93;</span></a></sup> or <a href="/wiki/Selective_receptor_modulator" title="Selective receptor modulator">selective receptor modulators</a>.<sup id="cite_ref-pmid14769827_8-0" class="reference"><a href="#cite_note-pmid14769827-8"><span class="cite-bracket">&#91;</span>8<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Mechanism_of_action">Mechanism of action</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=3" title="Edit section: Mechanism of action"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>As mentioned above, agonists have the potential to bind in different locations and in different ways depending on the type of agonist and the type of receptor.<sup id="cite_ref-:0_9-0" class="reference"><a href="#cite_note-:0-9"><span class="cite-bracket">&#91;</span>9<span class="cite-bracket">&#93;</span></a></sup> The process of binding is unique to the receptor-agonist relationship, but binding induces a conformational change and activates the receptor.<sup id="cite_ref-:0_9-1" class="reference"><a href="#cite_note-:0-9"><span class="cite-bracket">&#91;</span>9<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:1_10-0" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">&#91;</span>10<span class="cite-bracket">&#93;</span></a></sup> This conformational change is often the result of small changes in <a href="/wiki/Charge_density" title="Charge density">charge</a> or changes in <a href="/wiki/Protein_folding" title="Protein folding">protein folding</a> when the agonist is bound.<sup id="cite_ref-:1_10-1" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">&#91;</span>10<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:3_11-0" class="reference"><a href="#cite_note-:3-11"><span class="cite-bracket">&#91;</span>11<span class="cite-bracket">&#93;</span></a></sup> Two examples that demonstrate this process are the <a href="/wiki/Muscarinic_acetylcholine_receptor" title="Muscarinic acetylcholine receptor">muscarinic acetylcholine receptor</a> and <a href="/wiki/NMDA_receptor" title="NMDA receptor">NMDA receptor</a> and their respective agonists. </p> <figure class="mw-default-size mw-halign-left" typeof="mw:File/Thumb"><a href="/wiki/File:GPCR_Clipart.jpg" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/7/7d/GPCR_Clipart.jpg/220px-GPCR_Clipart.jpg" decoding="async" width="220" height="94" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/7/7d/GPCR_Clipart.jpg/330px-GPCR_Clipart.jpg 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/7/7d/GPCR_Clipart.jpg/440px-GPCR_Clipart.jpg 2x" data-file-width="590" data-file-height="253" /></a><figcaption>Simplified depiction of the mechanism of an agonist binding to a GPCR.</figcaption></figure> <p>For the <a href="/wiki/Muscarinic_acetylcholine_receptor" title="Muscarinic acetylcholine receptor">muscarinic acetylcholine receptor</a>, which is a <a href="/wiki/G_protein-coupled_receptor" title="G protein-coupled receptor">G protein-coupled receptor</a><sup id="cite_ref-:1_10-2" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">&#91;</span>10<span class="cite-bracket">&#93;</span></a></sup>(GPCR), the <a href="/wiki/Endogenous_agonist" title="Endogenous agonist">endogenous agonist</a> is <a href="/wiki/Acetylcholine" title="Acetylcholine">acetylcholine</a>. The binding of this <a href="/wiki/Neurotransmitter" title="Neurotransmitter">neurotransmitter</a> causes the conformational changes that propagate a signal into the cell.<sup id="cite_ref-:1_10-3" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">&#91;</span>10<span class="cite-bracket">&#93;</span></a></sup> The conformational changes are the primary effect of the agonist, and are related to the agonist's binding affinity and agonist <a href="/wiki/Efficacy" title="Efficacy">efficacy</a>.<sup id="cite_ref-:0_9-2" class="reference"><a href="#cite_note-:0-9"><span class="cite-bracket">&#91;</span>9<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:2_12-0" class="reference"><a href="#cite_note-:2-12"><span class="cite-bracket">&#91;</span>12<span class="cite-bracket">&#93;</span></a></sup> Other agonists that bind to this receptor will fall under one of the different categories of agonist mentioned above based on their specific binding affinity and efficacy. </p> <figure class="mw-default-size mw-halign-left" typeof="mw:File/Thumb"><a href="/wiki/File:Co-agonist_Simple.jpg" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/c/ca/Co-agonist_Simple.jpg/220px-Co-agonist_Simple.jpg" decoding="async" width="220" height="87" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/c/ca/Co-agonist_Simple.jpg/330px-Co-agonist_Simple.jpg 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/c/ca/Co-agonist_Simple.jpg/440px-Co-agonist_Simple.jpg 2x" data-file-width="483" data-file-height="191" /></a><figcaption>Simplified depiction of co-agonists activating a receptor.</figcaption></figure> <p>The <a href="/wiki/NMDA_receptor" title="NMDA receptor">NMDA receptor</a> is an example of an alternate mechanism of action, as the NMDA receptor requires co-agonists for activation. Rather than simply requiring a single specific agonist, the NMDA receptor requires both the <a href="/wiki/Endogenous_agonist" title="Endogenous agonist">endogenous agonists</a>, <a href="/wiki/N-Methyl-D-aspartic_acid" title="N-Methyl-D-aspartic acid">N-methyl-D-aspartate</a> (NMDA) and <a href="/wiki/Glycine" title="Glycine">glycine</a>.<sup id="cite_ref-:3_11-1" class="reference"><a href="#cite_note-:3-11"><span class="cite-bracket">&#91;</span>11<span class="cite-bracket">&#93;</span></a></sup> These co-agonists are both required to induce the conformational change needed for the NMDA receptor to allow flow through the <a href="/wiki/Ion_channel" title="Ion channel">ion channel</a>, in this case calcium.<sup id="cite_ref-:3_11-2" class="reference"><a href="#cite_note-:3-11"><span class="cite-bracket">&#91;</span>11<span class="cite-bracket">&#93;</span></a></sup> An aspect demonstrated by the NMDA receptor is that the mechanism or response of agonists can be blocked by a variety of chemical and biological factors.<sup id="cite_ref-:3_11-3" class="reference"><a href="#cite_note-:3-11"><span class="cite-bracket">&#91;</span>11<span class="cite-bracket">&#93;</span></a></sup> NMDA receptors specifically are blocked by a <a href="/wiki/Magnesium" title="Magnesium">magnesium</a> ion unless the cell is also experiencing <a href="/wiki/Depolarization" title="Depolarization">depolarization</a>.<sup id="cite_ref-:3_11-4" class="reference"><a href="#cite_note-:3-11"><span class="cite-bracket">&#91;</span>11<span class="cite-bracket">&#93;</span></a></sup> </p><p>These differences show that agonists have unique mechanisms of action depending on the receptor activated and the response needed.<sup id="cite_ref-:0_9-3" class="reference"><a href="#cite_note-:0-9"><span class="cite-bracket">&#91;</span>9<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:1_10-4" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">&#91;</span>10<span class="cite-bracket">&#93;</span></a></sup> The goal and process remains generally consistent however, with the primary mechanism of action requiring the binding of the agonist and the subsequent changes in conformation to cause the desired response at the receptor.<sup id="cite_ref-:0_9-4" class="reference"><a href="#cite_note-:0-9"><span class="cite-bracket">&#91;</span>9<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:2_12-1" class="reference"><a href="#cite_note-:2-12"><span class="cite-bracket">&#91;</span>12<span class="cite-bracket">&#93;</span></a></sup> This response as discussed above can vary from allowing flow of <a href="/wiki/Ion" title="Ion">ions</a> to activating a <a href="/wiki/G_protein-coupled_receptor" title="G protein-coupled receptor">GPCR</a> and transmitting a signal into the <a href="/wiki/Cell_(biology)" title="Cell (biology)">cell</a>.<sup id="cite_ref-:0_9-5" class="reference"><a href="#cite_note-:0-9"><span class="cite-bracket">&#91;</span>9<span class="cite-bracket">&#93;</span></a></sup><sup id="cite_ref-:1_10-5" class="reference"><a href="#cite_note-:1-10"><span class="cite-bracket">&#91;</span>10<span class="cite-bracket">&#93;</span></a></sup> </p> <div class="mw-heading mw-heading2"><h2 id="Activity">Activity</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=4" title="Edit section: Activity"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <figure class="mw-halign-right" typeof="mw:File/Thumb"><a href="/wiki/File:Efficacy_spectrum.png" class="mw-file-description"><img src="//upload.wikimedia.org/wikipedia/commons/thumb/b/bd/Efficacy_spectrum.png/320px-Efficacy_spectrum.png" decoding="async" width="320" height="123" class="mw-file-element" srcset="//upload.wikimedia.org/wikipedia/commons/thumb/b/bd/Efficacy_spectrum.png/480px-Efficacy_spectrum.png 1.5x, //upload.wikimedia.org/wikipedia/commons/thumb/b/bd/Efficacy_spectrum.png/640px-Efficacy_spectrum.png 2x" data-file-width="2436" data-file-height="937" /></a><figcaption>Efficacy spectrum of receptor ligands.</figcaption></figure> <div class="mw-heading mw-heading3"><h3 id="Potency">Potency</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=5" title="Edit section: Potency"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>Potency is the amount of agonist needed to elicit a desired response. The <a href="/wiki/Potency_(pharmacology)" title="Potency (pharmacology)">potency</a> of an agonist is inversely related to its <a href="/wiki/Half_maximal_effective_concentration" class="mw-redirect" title="Half maximal effective concentration">half maximal effective concentration</a> (EC<sub>50</sub>) value. The EC<sub>50</sub> can be measured for a given agonist by determining the concentration of agonist needed to elicit half of the maximum biological response of the agonist. The EC<sub>50</sub> value is useful for comparing the potency of drugs with similar <a href="/wiki/Efficacy#Pharmacology" title="Efficacy">efficacies</a> producing physiologically similar effects. The smaller the EC<sub>50</sub> value, the greater the potency of the agonist, the lower the concentration of drug that is required to elicit the maximum biological response. </p> <div class="mw-heading mw-heading3"><h3 id="Therapeutic_index">Therapeutic index</h3><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=6" title="Edit section: Therapeutic index"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <p>When a drug is used therapeutically, it is important to understand the margin of safety that exists between the dose needed for the desired effect and the dose that produces unwanted and possibly dangerous side-effects (measured by the TD<sub>50</sub>, the dose that produces toxicity in 50% of individuals). This relationship, termed the <a href="/wiki/Therapeutic_index" title="Therapeutic index">therapeutic index</a>, is defined as the ratio <a href="/wiki/Median_toxic_dose" title="Median toxic dose">TD<sub>50</sub></a>:<a href="/wiki/Effective_dose_(pharmacology)" title="Effective dose (pharmacology)">ED<sub>50</sub></a>. In general, the narrower this margin, the more likely it is that the drug will produce unwanted effects. The therapeutic index emphasizes the importance of the margin of safety, as distinct from the potency, in determining the usefulness of a drug. </p> <div class="mw-heading mw-heading2"><h2 id="See_also">See also</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=7" title="Edit section: See also"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <ul><li><a href="/wiki/Allosteric_regulation#Pharmacology" title="Allosteric regulation">Allosteric modulator</a></li> <li><a href="/wiki/Dose_response_curve" class="mw-redirect" title="Dose response curve">Dose response curve</a></li> <li><a href="/wiki/Excitatory_postsynaptic_potential" title="Excitatory postsynaptic potential">Excitatory postsynaptic potential</a></li> <li><a href="/wiki/Functional_selectivity" title="Functional selectivity">Functional selectivity</a></li> <li><a href="/wiki/Intrinsic_activity" title="Intrinsic activity">Intrinsic activity</a></li> <li><a href="/wiki/Inverse_agonist" title="Inverse agonist">Inverse agonist</a></li> <li><a href="/wiki/Mixed_agonist/antagonist" class="mw-redirect" title="Mixed agonist/antagonist">Mixed agonist/antagonist</a></li> <li><a href="/wiki/Receptor_antagonist" title="Receptor antagonist">Receptor antagonist</a></li> <li><a href="/wiki/Receptor_theory" title="Receptor theory">Receptor theory</a></li></ul> <div class="mw-heading mw-heading2"><h2 id="References">References</h2><span class="mw-editsection"><span class="mw-editsection-bracket">[</span><a href="/w/index.php?title=Agonist&amp;action=edit&amp;section=8" title="Edit section: References"><span>edit</span></a><span class="mw-editsection-bracket">]</span></span></div> <div class="mw-references-wrap mw-references-columns"><ol class="references"> <li id="cite_note-1"><span class="mw-cite-backlink"><b><a href="#cite_ref-1">^</a></b></span> <span class="reference-text">Goodman and Gilman's Manual of Pharmacology and Therapeutics. (11th edition, 2008). p14. <style data-mw-deduplicate="TemplateStyles:r1238218222">.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.id-lock-free a{background:url("//upload.wikimedia.org/wikipedia/commons/6/65/Lock-green.svg")right 0.1em center/9px no-repeat}.mw-parser-output .id-lock-limited.id-lock-limited a,.mw-parser-output .id-lock-registration.id-lock-registration a{background: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.id-lock-subscription a{background: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:url("//upload.wikimedia.org/wikipedia/commons/4/4c/Wikisource-logo.svg")right 0.1em center/12px no-repeat}body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-free a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-limited a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-registration a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .id-lock-subscription a,body:not(.skin-timeless):not(.skin-minerva) .mw-parser-output .cs1-ws-icon a{background-size:contain;padding:0 1em 0 0}.mw-parser-output .cs1-code{color:inherit;background:inherit;border:none;padding:inherit}.mw-parser-output .cs1-hidden-error{display:none;color:var(--color-error,#d33)}.mw-parser-output .cs1-visible-error{color:var(--color-error,#d33)}.mw-parser-output .cs1-maint{display:none;color:#085;margin-left:0.3em}.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}@media screen{.mw-parser-output .cs1-format{font-size:95%}html.skin-theme-clientpref-night .mw-parser-output .cs1-maint{color:#18911f}}@media screen and (prefers-color-scheme:dark){html.skin-theme-clientpref-os .mw-parser-output .cs1-maint{color:#18911f}}</style><a href="/wiki/ISBN_(identifier)" class="mw-redirect" title="ISBN (identifier)">ISBN</a>&#160;<a href="/wiki/Special:BookSources/0-07-144343-6" title="Special:BookSources/0-07-144343-6">0-07-144343-6</a></span> </li> <li id="cite_note-2"><span class="mw-cite-backlink"><b><a href="#cite_ref-2">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFDe_Mey_JGRCompeerMeens2009" class="citation journal cs1">De Mey JGR, Compeer MG, Meens MJ (2009). "Endothelin-1, an Endogenous Irreversible Agonist in Search of an Allosteric Inhibitor". <i>Mol Cell Pharmacol</i>. <b>1</b> (5): 246–257.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=article&amp;rft.jtitle=Mol+Cell+Pharmacol&amp;rft.atitle=Endothelin-1%2C+an+Endogenous+Irreversible+Agonist+in+Search+of+an+Allosteric+Inhibitor&amp;rft.volume=1&amp;rft.issue=5&amp;rft.pages=246-257&amp;rft.date=2009&amp;rft.au=De+Mey+JGR&amp;rft.au=Compeer%2C+MG&amp;rft.au=Meens%2C+MJ&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AAgonist" class="Z3988"></span></span> </li> <li id="cite_note-3"><span class="mw-cite-backlink"><b><a href="#cite_ref-3">^</a></b></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFRosenbaumZhangLyonsHoll2011" class="citation journal cs1">Rosenbaum DM, Zhang C, Lyons JA, Holl R, Aragao D, Arlow DH, et&#160;al. 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class="Z3988"></span></span> </li> <li id="cite_note-:3-11"><span class="mw-cite-backlink">^ <a href="#cite_ref-:3_11-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-:3_11-1"><sup><i><b>b</b></i></sup></a> <a href="#cite_ref-:3_11-2"><sup><i><b>c</b></i></sup></a> <a href="#cite_ref-:3_11-3"><sup><i><b>d</b></i></sup></a> <a href="#cite_ref-:3_11-4"><sup><i><b>e</b></i></sup></a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFZhuSteinYoshiokaLee2016" class="citation journal cs1">Zhu S, Stein RA, Yoshioka C, Lee CH, Goehring A, Mchaourab HS, Gouaux E (April 2016). <a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4914038">"Mechanism of NMDA Receptor Inhibition and Activation"</a>. <i>Cell</i>. <b>165</b> (3): 704–714. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.1016%2Fj.cell.2016.03.028">10.1016/j.cell.2016.03.028</a>. <a href="/wiki/PMC_(identifier)" class="mw-redirect" title="PMC (identifier)">PMC</a>&#160;<span class="id-lock-free" title="Freely accessible"><a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4914038">4914038</a></span>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a>&#160;<a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/27062927">27062927</a>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=article&amp;rft.jtitle=Cell&amp;rft.atitle=Mechanism+of+NMDA+Receptor+Inhibition+and+Activation&amp;rft.volume=165&amp;rft.issue=3&amp;rft.pages=704-714&amp;rft.date=2016-04&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC4914038%23id-name%3DPMC&amp;rft_id=info%3Apmid%2F27062927&amp;rft_id=info%3Adoi%2F10.1016%2Fj.cell.2016.03.028&amp;rft.aulast=Zhu&amp;rft.aufirst=S&amp;rft.au=Stein%2C+RA&amp;rft.au=Yoshioka%2C+C&amp;rft.au=Lee%2C+CH&amp;rft.au=Goehring%2C+A&amp;rft.au=Mchaourab%2C+HS&amp;rft.au=Gouaux%2C+E&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC4914038&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AAgonist" class="Z3988"></span></span> </li> <li id="cite_note-:2-12"><span class="mw-cite-backlink">^ <a href="#cite_ref-:2_12-0"><sup><i><b>a</b></i></sup></a> <a href="#cite_ref-:2_12-1"><sup><i><b>b</b></i></sup></a></span> <span class="reference-text"><link rel="mw-deduplicated-inline-style" href="mw-data:TemplateStyles:r1238218222"><cite id="CITEREFStrange2008" class="citation journal cs1">Strange PG (April 2008). <a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2437915">"Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors"</a>. <i>British Journal of Pharmacology</i>. <b>153</b> (7): 1353–1363. <a href="/wiki/Doi_(identifier)" class="mw-redirect" title="Doi (identifier)">doi</a>:<a rel="nofollow" class="external text" href="https://doi.org/10.1038%2Fsj.bjp.0707672">10.1038/sj.bjp.0707672</a>. <a href="/wiki/PMC_(identifier)" class="mw-redirect" title="PMC (identifier)">PMC</a>&#160;<span class="id-lock-free" title="Freely accessible"><a rel="nofollow" class="external text" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2437915">2437915</a></span>. <a href="/wiki/PMID_(identifier)" class="mw-redirect" title="PMID (identifier)">PMID</a>&#160;<a rel="nofollow" class="external text" href="https://pubmed.ncbi.nlm.nih.gov/18223670">18223670</a>.</cite><span title="ctx_ver=Z39.88-2004&amp;rft_val_fmt=info%3Aofi%2Ffmt%3Akev%3Amtx%3Ajournal&amp;rft.genre=article&amp;rft.jtitle=British+Journal+of+Pharmacology&amp;rft.atitle=Agonist+binding%2C+agonist+affinity+and+agonist+efficacy+at+G+protein-coupled+receptors&amp;rft.volume=153&amp;rft.issue=7&amp;rft.pages=1353-1363&amp;rft.date=2008-04&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC2437915%23id-name%3DPMC&amp;rft_id=info%3Apmid%2F18223670&amp;rft_id=info%3Adoi%2F10.1038%2Fsj.bjp.0707672&amp;rft.aulast=Strange&amp;rft.aufirst=PG&amp;rft_id=https%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fpmc%2Farticles%2FPMC2437915&amp;rfr_id=info%3Asid%2Fen.wikipedia.org%3AAgonist" class="Z3988"></span></span> </li> </ol></div> <div class="navbox-styles"><style data-mw-deduplicate="TemplateStyles:r1129693374">.mw-parser-output .hlist dl,.mw-parser-output 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abbr{color:var(--color-base)!important}}@media print{.mw-parser-output .navbar{display:none!important}}</style><div class="navbar plainlinks hlist navbar-mini"><ul><li class="nv-view"><a href="/wiki/Template:Pharmacology" title="Template:Pharmacology"><abbr title="View this template">v</abbr></a></li><li class="nv-talk"><a href="/wiki/Template_talk:Pharmacology" title="Template talk:Pharmacology"><abbr title="Discuss this template">t</abbr></a></li><li class="nv-edit"><a href="/wiki/Special:EditPage/Template:Pharmacology" title="Special:EditPage/Template:Pharmacology"><abbr title="Edit this template">e</abbr></a></li></ul></div><div id="Pharmacology" style="font-size:114%;margin:0 4em"><a href="/wiki/Pharmacology" title="Pharmacology">Pharmacology</a></div></th></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Ligand_(biochemistry)" title="Ligand (biochemistry)">Ligand (biochemistry)</a></th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Excitatory" scope="row" class="navbox-group" style="width:1%;text-align: center;">Excitatory</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a class="mw-selflink selflink">Agonist</a></li> <li><a href="/wiki/Endogenous_agonist" title="Endogenous agonist">Endogenous agonist</a></li> <li><a href="/wiki/Irreversible_agonist" title="Irreversible agonist">Irreversible agonist</a></li> <li><a href="/wiki/Partial_agonist" title="Partial agonist">Partial agonist</a></li> <li><a href="/wiki/Superagonist" title="Superagonist">Superagonist</a></li> <li><a href="/wiki/Physiological_agonism_and_antagonism" title="Physiological agonism and antagonism">Physiological agonist</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Inhibitory" scope="row" class="navbox-group" style="width:1%;text-align: center;">Inhibitory</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Receptor_antagonist" title="Receptor antagonist">Antagonist</a></li> <li><a href="/wiki/Competitive_antagonist" class="mw-redirect" title="Competitive antagonist">Competitive antagonist</a></li> <li><a href="/wiki/Irreversible_antagonist" title="Irreversible antagonist">Irreversible antagonist</a></li> <li><a href="/wiki/Physiological_agonism_and_antagonism" title="Physiological agonism and antagonism">Physiological antagonist</a></li> <li><a href="/wiki/Inverse_agonist" title="Inverse agonist">Inverse agonist</a></li> <li><a href="/wiki/Enzyme_inhibitor" title="Enzyme inhibitor">Enzyme inhibitor</a></li></ul> </div></td></tr></tbody></table><div> <ul><li><a href="/wiki/Drug" title="Drug">Drug</a></li> <li><a href="/wiki/Neurotransmitter" title="Neurotransmitter">Neurotransmitter</a></li> <li><a href="/wiki/Agonist-antagonist" title="Agonist-antagonist">Agonist-antagonist</a></li> <li><a href="/wiki/Pharmacophore" title="Pharmacophore">Pharmacophore</a></li></ul></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Pharmacodynamics" title="Pharmacodynamics">Pharmacodynamics</a></th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Activity_at_receptor" scope="row" class="navbox-group" style="width:1%;text-align: center;">Activity at receptor</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <li><a href="/wiki/Mechanism_of_action" title="Mechanism of action">Mechanism of action</a></li> <li><a href="/wiki/Mode_of_action" title="Mode of action">Mode of action</a></li> <li><a href="/wiki/Molecular_binding" title="Molecular binding">Binding</a></li> <li><a href="/wiki/Receptor_(biochemistry)" title="Receptor (biochemistry)">Receptor (biochemistry)</a></li> <li><a href="/wiki/Desensitization_(medicine)" title="Desensitization (medicine)">Desensitization (medicine)</a></li> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Other_effects_of_ligand" scope="row" class="navbox-group" style="width:1%;text-align: center;">Other effects of ligand</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li>Selectivity (<a href="/wiki/Binding_selectivity" title="Binding selectivity">Binding</a>, <a href="/wiki/Functional_selectivity" title="Functional selectivity">Functional</a>)</li> <li><a href="/wiki/Pleiotropy_(drugs)" title="Pleiotropy (drugs)">Pleiotropy (drugs)</a></li> <li><a href="/wiki/Non-specific_effect_of_vaccines" title="Non-specific effect of vaccines">Non-specific effect of vaccines</a></li> <li><a href="/wiki/Adverse_effect" title="Adverse effect">Adverse effect</a></li> <li><a href="/wiki/Toxicity" title="Toxicity">Toxicity</a> (<a href="/wiki/Neurotoxicity" title="Neurotoxicity">Neurotoxicity</a>)</li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Analysis" scope="row" class="navbox-group" style="width:1%;text-align: center;">Analysis</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Dose%E2%80%93response_relationship" title="Dose–response relationship">Dose–response relationship</a></li> <li><a href="/wiki/Hill_equation_(biochemistry)" title="Hill equation (biochemistry)">Hill equation (biochemistry)</a></li> <li><a href="/wiki/Schild_plot" class="mw-redirect" title="Schild plot">Schild plot</a></li> <li><a href="/wiki/Del_Castillo_Katz_model" class="mw-redirect" title="Del Castillo Katz model">Del Castillo Katz model</a></li> <li><a href="/wiki/Cheng-Prussoff_Equation" class="mw-redirect" title="Cheng-Prussoff Equation">Cheng-Prussoff Equation</a></li> <li>Methods (<a href="/wiki/Organ_bath" title="Organ bath">Organ bath</a>, <a href="/wiki/Ligand_binding_assay" title="Ligand binding assay">Ligand binding assay</a>, <a href="/wiki/Patch_clamp" title="Patch clamp">Patch clamp</a>)</li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Metrics" scope="row" class="navbox-group" style="width:1%;text-align: center;">Metrics</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Efficacy#Pharmacology" title="Efficacy">Efficacy</a></li> <li><a href="/wiki/Intrinsic_activity" title="Intrinsic activity">Intrinsic activity</a></li> <li><a href="/wiki/Potency_(pharmacology)" title="Potency (pharmacology)">Potency</a> (<a href="/wiki/EC50" title="EC50">EC50</a>, <a href="/wiki/IC50" title="IC50">IC50</a>, <a href="/wiki/Effective_dose_(pharmacology)" title="Effective dose (pharmacology)">ED50</a>, <a href="/wiki/Median_lethal_dose" title="Median lethal dose">LD50</a>, <a href="/wiki/Median_toxic_dose" title="Median toxic dose">TD50</a>)</li> <li><a href="/wiki/Therapeutic_index" title="Therapeutic index">Therapeutic index</a></li> <li><a href="/wiki/Dissociation_constant#Protein-ligand_binding" title="Dissociation constant">Affinity</a></li></ul> </div></td></tr></tbody></table><div></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Pharmacokinetics" title="Pharmacokinetics">Pharmacokinetics</a></th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Metrics" scope="row" class="navbox-group" style="width:1%;text-align: center;">Metrics</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Loading_dose" title="Loading dose">Loading dose</a></li> <li><a href="/wiki/Volume_of_distribution" title="Volume of distribution">Volume of distribution</a> (<a href="/wiki/Initial_volume_of_distribution" title="Initial volume of distribution">Initial</a>)</li> <li><a href="/wiki/Rate_of_infusion" title="Rate of infusion">Rate of infusion</a></li> <li><a href="/wiki/Onset_of_action" title="Onset of action">Onset of action</a></li> <li><a href="/wiki/Biological_half-life" title="Biological half-life">Biological half-life</a></li> <li><a href="/wiki/Plasma_protein_binding" title="Plasma protein binding">Plasma protein binding</a></li> <li><a href="/wiki/Bioavailability" title="Bioavailability">Bioavailability</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="LADME" scope="row" class="navbox-group" style="width:1%;text-align: center;">LADME</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/ADME" title="ADME">(L)ADME</a>: (<a href="/wiki/Liberation_(pharmacology)" title="Liberation (pharmacology)">Liberation</a>)</li> <li><a href="/wiki/Absorption_(pharmacology)" title="Absorption (pharmacology)">Absorption</a></li> <li><a href="/wiki/Distribution_(pharmacology)" title="Distribution (pharmacology)">Distribution</a></li> <li><a href="/wiki/Drug_metabolism" title="Drug metabolism">Metabolism</a></li> <li><a href="/wiki/Excretion" title="Excretion">Excretion</a> (<a href="/wiki/Clearance_(pharmacology)" title="Clearance (pharmacology)">Clearance</a>)</li></ul> </div></td></tr></tbody></table><div> <ul><li><a href="/wiki/Compartment_(pharmacokinetics)" title="Compartment (pharmacokinetics)">Compartment</a></li> <li><a href="/wiki/Bioequivalence" title="Bioequivalence">Bioequivalence</a></li></ul></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;">Related<br /> fields</th><td class="navbox-list-with-group navbox-list navbox-odd hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"></div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Neuroscience_and_psychology" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Neuroscience" title="Neuroscience">Neuroscience</a> and <a href="/wiki/Psychology" title="Psychology">psychology</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <li><a href="/wiki/Neuropsychopharmacology" title="Neuropsychopharmacology">Neuropsychopharmacology</a></li> <li><a href="/wiki/Neuropharmacology" title="Neuropharmacology">Neuropharmacology</a></li> <li><a href="/wiki/Psychopharmacology" title="Psychopharmacology">Psychopharmacology</a></li> <li><a href="/wiki/Electrophysiology" title="Electrophysiology">Electrophysiology</a></li> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Medicine" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Medicine" title="Medicine">Medicine</a></th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Clinical_pharmacology" title="Clinical pharmacology">Clinical pharmacology</a></li> <li><a href="/wiki/Pharmacy" title="Pharmacy">Pharmacy</a></li> <li><a href="/wiki/Medicinal_chemistry" title="Medicinal chemistry">Medicinal chemistry</a></li> <li><a href="/wiki/Pharmacoepidemiology" title="Pharmacoepidemiology">Pharmacoepidemiology</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Biochemistry_and_genetics" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Biochemistry" title="Biochemistry">Biochemistry</a> and <a href="/wiki/Genetics" title="Genetics">genetics</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Pharmacoinformatics" title="Pharmacoinformatics">Pharmacoinformatics</a></li> <li><a href="/wiki/Pharmacogenetics" class="mw-redirect" title="Pharmacogenetics">Pharmacogenetics</a></li> <li><a href="/wiki/Pharmacogenomics" title="Pharmacogenomics">Pharmacogenomics</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Toxicology" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Toxicology" title="Toxicology">Toxicology</a></th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Pharmacotoxicology" title="Pharmacotoxicology">Pharmacotoxicology</a></li> <li><a href="/wiki/Neurotoxicology" class="mw-redirect" title="Neurotoxicology">Neurotoxicology</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Drug_discovery" scope="row" class="navbox-group" style="width:1%;text-align: center;"><a href="/wiki/Drug_discovery" title="Drug discovery">Drug discovery</a></th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Classical_pharmacology" title="Classical pharmacology">Classical pharmacology</a></li> <li><a href="/wiki/Reverse_pharmacology" title="Reverse pharmacology">Reverse pharmacology</a></li></ul> </div></td></tr></tbody></table><div> <ul><li><a href="/wiki/Photopharmacology" title="Photopharmacology">Photopharmacology</a></li> <li><a href="/wiki/Immunopharmacology" class="mw-redirect" title="Immunopharmacology">Immunopharmacology</a></li> <li><a href="/wiki/Cell_biology" title="Cell biology">Cell biology</a></li> <li><a href="/wiki/Physiology" title="Physiology">Physiology</a></li></ul></div></td></tr><tr><th scope="row" class="navbox-group" style="width:1%;text-align: center;">Other</th><td class="navbox-list-with-group navbox-list navbox-even hlist" style="width:100%;padding:0"><div style="padding:0 0.25em"> <li><a href="/wiki/Coinduction_(anesthetics)" title="Coinduction (anesthetics)">Coinduction (anesthetics)</a></li> <li><a href="/wiki/Combination_therapy" title="Combination therapy">Combination therapy</a></li> <li><a href="/wiki/Functional_analog_(chemistry)" title="Functional analog (chemistry)">Functional analog (chemistry)</a></li> <li><a href="/wiki/Polypharmacology" title="Polypharmacology">Polypharmacology</a></li> <li><a href="/wiki/Chemotherapy" title="Chemotherapy">Chemotherapy</a></li> <li><a href="/wiki/Lists_of_drugs" title="Lists of drugs">Lists of drugs</a></li> <li><a href="/wiki/WHO_list_of_essential_medicines" class="mw-redirect" title="WHO list of essential medicines">WHO list of essential medicines</a></li> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Tolerance_and_resistance" scope="row" class="navbox-group" style="width:1%;text-align: center;">Tolerance and resistance</th><td class="navbox-list-with-group navbox-list navbox-odd" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Drug_tolerance" title="Drug tolerance">Drug tolerance</a></li> <li><a href="/wiki/Tachyphylaxis" title="Tachyphylaxis">Tachyphylaxis</a></li> <li><a href="/wiki/Drug_resistance" title="Drug resistance">Drug resistance</a></li> <li><a href="/wiki/Antibiotic_resistance" class="mw-redirect" title="Antibiotic resistance">Antibiotic resistance</a></li> <li><a href="/wiki/Multiple_drug_resistance" title="Multiple drug resistance">Multiple drug resistance</a></li></ul> </div></td></tr></tbody></table><div> </div><table class="nowraplinks navbox-subgroup" style="border-spacing:0"><tbody><tr><th id="Antimicrobial_pharmacology" scope="row" class="navbox-group" style="width:1%;text-align: center;">Antimicrobial pharmacology</th><td class="navbox-list-with-group navbox-list navbox-even" style="width:100%;padding:0"><div style="padding:0 0.25em"> <ul><li><a href="/wiki/Antimicrobial_pharmacodynamics" title="Antimicrobial pharmacodynamics">Antimicrobial pharmacodynamics</a></li> <li><a href="/wiki/Minimum_inhibitory_concentration" title="Minimum inhibitory concentration">Minimum inhibitory concentration</a></li> <li><a href="/wiki/Bacteriostatic_agent" title="Bacteriostatic agent">Bacteriostatic</a></li> <li><a href="/wiki/Minimum_bactericidal_concentration" title="Minimum bactericidal concentration">Minimum bactericidal concentration</a></li> <li><a href="/wiki/Bactericide" title="Bactericide">Bactericide</a></li></ul> </div></td></tr></tbody></table><div> </div></td></tr></tbody></table></div> <!-- NewPP limit report Parsed by mw‐web.codfw.main‐f69cdc8f6‐7g25x Cached time: 20241122141052 Cache expiry: 2592000 Reduced expiry: false Complications: [vary‐revision‐sha1, show‐toc] CPU time usage: 0.437 seconds Real time usage: 0.558 seconds Preprocessor visited node count: 1594/1000000 Post‐expand include size: 83199/2097152 bytes Template argument size: 1318/2097152 bytes Highest 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