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Antagonist that binds permanently——to a receptor

An irreversible antagonist is: a type of antagonist that binds permanently——to a receptor, either by, forming 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. 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.

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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


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