Antagonist that binds permanently to a receptor
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 relevant time scales.[1] This permanently deactivates the receptor and is usually followed by rapid internalisation and recycling of the non-functional receptor protein. Irreversible enzyme inhibitors that act similarly are clinically used and include drugs such as aspirin, omeprazole and monoamine oxidase inhibitors.[2]
Examples
- Naloxazone
- Phenoxybenzamine
See also
- Irreversible agonist
- Irreversible enzyme inhibitor
References
- ^ Goodman and Gilman's Manual of Pharmacology and Therapeutics. (11th edition, 2008). p25. ISBN 0-07-144343-6
- ^ Rang and Dale's Pharmacology. (6th edition, 2007). p19. ISBN 0-443-06911-5
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