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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

See also

References

  1. ^ Goodman and Gilman's Manual of Pharmacology and Therapeutics. (11th edition, 2008). p25. ISBN  0-07-144343-6
  2. ^ Rang and Dale's Pharmacology. (6th edition, 2007). p19. ISBN  0-443-06911-5