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 (reversible) 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.
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.
Examples
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Oxymorphazone
Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound. This g ...
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Metaphit
Metaphit (1- -(3-Isothiocyanato)phenylyclohexylpiperidine) is a research chemical that acts as an acylator of NMDARAn, sigma and DAT binding sites in the CNS. It is the ''m''-isothiocyanate derivative of phencyclidine (PCP) and binds irreversi ...
See also
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Agonist
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Irreversible antagonist
An irreversible antagonist is a type of antagonist that binds permanently to a receptor, either by forming a covalent bond to the active site, or alternatively just by binding so tightly that the rate of dissociation is effectively zero at rele ...
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Irreversible enzyme inhibitor
References
Receptor agonists
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