Receptor antagonist

<p>A receptor antagonist is a type of  <a href="/facts/Receptor_(biochemistry)/tjTAC76a">receptor</a> <a href="/facts/Ligand_(biochemistry)/44QLL4eU">ligand</a> or <a href="/facts/Drug/FFFUI9n4">drug</a> that blocks or dampens a biological response by binding to and blocking a <a href="/facts/Receptor_(biochemistry)/tjTAC76a">receptor</a> rather than activating it like an <a href="/facts/Agonist/nz8U5NNp">agonist</a>. Antagonist drugs interfere in the natural operation of receptor proteins. They are sometimes called blockers; examples include <a href="/facts/Alpha_blocker/MqNLhfS9">alpha blockers</a>, <a href="/facts/Beta_blocker/PRsWgpLV">beta blockers</a>, and <a href="/facts/Calcium_channel_blocker/st91pD2K">calcium channel blockers</a>. In <a href="/facts/Pharmacology/4Rx8s7Ie">pharmacology</a>, antagonists have <a href="/facts/Binding_affinity/44QLL4eU">affinity</a> but no <a href="/facts/Efficacy/PNlTeDtD">efficacy</a> for their cognate receptors, and binding will disrupt the interaction and inhibit the function of an <a href="/facts/Agonist/nz8U5NNp">agonist</a> or <a href="/facts/Inverse_agonist/NDLoA789">inverse agonist</a> at receptors. Antagonists mediate their effects by binding to the <a href="/facts/Active_site/u9ua7rGu">active site</a> or to the <a href="/facts/Allosteric_regulation/alMRuyt9">allosteric site</a> on a receptor, or they may interact at unique binding sites not normally involved in the biological regulation of the receptor's activity. Antagonist activity may be reversible or irreversible depending on the longevity of the antagonist–receptor complex, which, in turn, depends on the nature of antagonist–receptor binding. The majority of drug antagonists achieve their potency by competing with endogenous ligands or substrates at structurally defined binding sites on receptors.
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Receptor antagonist open-in-new

Receptor antagonist