This article needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. Find sources: "Irreversible agonist" – news · newspapers · books · scholar · JSTOR(January 2013) (Learn how and when to remove this message)
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.[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.
^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
and 25 Related for: Irreversible agonist information
An irreversibleagonist is a type of agonist that binds permanently to a receptor in such a manner that the receptor is permanently activated. It is distinct...
agonist for the target receptor. It might be argued that the endogenous agonist is simply a partial agonist in that tissue. An irreversibleagonist is...
and irreversible antagonist drugs, as effects of non-competitive antagonists are reversible and activity of agonist will be restored. Irreversible competitive...
higher concentration of inhibitor leads to lowered agonist activity. IC50 value increases as agonist concentration increases. Furthermore, depending on...
oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it...
Chlornaltrexamine is an irreversible mixed agonist–antagonist for μ-opioid receptors, which forms a covalent bond to the binding site. It is 22 times more...
Chloroxymorphamine is an opioid and a derivative of oxymorphone which binds irreversibly as an agonist to the μ-opioid receptor. Chlornaltrexamine Naloxazone Oxymorphazone...
Chloroethylclonidine is an irreversibleagonist for adrenergic receptors, in particular alpha1B, D, C and alpha2A/D-subtypes. Docherty JR, O'Rourke M (February...
formerly Vivalan) – also a 5-HT2B receptor antagonist and 5-HT2C receptor agonist Atomoxetine (Strattera) Bupropion (Wellbutrin, Elontril) – also a non-competitive...
Gmeiner P, Kobilka BK (January 2011). "Structure and function of an irreversibleagonist-β(2) adrenoceptor complex". Nature. 469 (7329): 236–40. Bibcode:2011Natur...
different subtypes of agonists, including endogenous agonists, super agonist, full agonist, inverse agonist, and irreversibleagonist. Radioligands are made...
is the m-isothiocyanate derivative of phencyclidine (PCP) and binds irreversibly (forming a covalent bond) to the PCP binding site on the NMDA receptor...
antagonist. An irreversible antagonist binds so strongly to the receptor as to render the receptor unavailable for binding to the agonist. Irreversible antagonists...
inhibitors are classified as reversible, irreversible, or quasi-irreversible (also called pseudo-irreversible). Organophosphates like TEPP and sarin inhibit...
Zhang; Joseph A. Lyons; et al. (2011). "Structure and function of an irreversibleagonist-β2 adrenoceptor complex". Nature. 469 (7329): 236–240. Bibcode:2011Natur...
impairments were reversed when treated with physostigmine, a cholinergic agonist. However, reversing memory impairments in AD patients may not be this easy...
type of opioid receptor, it may be an agonist, partial agonist, or antagonist. Buprenorphine's activity as an agonist/antagonist is important in the treatment...
of FSCPX, an irreversible A(1) adenosine receptor antagonist, on the negative inotropic action of A(1) adenosine receptor full agonists in isolated guinea...
Global Information