Irreversible agonist

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An irreversible agonist is a type of agonist that binds permanently to a receptor in such a manner that the receptor is permanently activated. It is distinct from a mere agonist in that the association of an agonist to a receptor is reversible, whereas the binding of an irreversible agonist to a receptor is, at least in theory, irreversible. Oxymorphazone is an example of an irreversible agonist.[1] In practice, the distinction may be more a matter of degree, in which the binding affinity of an irreversible agonist is some orders of magnitude greater than that of an agonist.

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  1. ^ Galetta S, Ling GS, Wolfin L, Pasternak GW (Sep 1982), "Receptor binding and analgesic properties of oxymorphazone", Life Sciences 31 (12-13): 1389–92, doi:10.1016/0024-3205(82)90388-5, PMID 6183551