Partial agonist

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Agonists

Partial agonists (such as buspirone, aripiprazole, buprenorphine, or norclozapine) also bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects - when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone.1 Clinically partial agonists can activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present.2

See also

Intrinsic sympathomimetic activity of Beta-blockers.

References

  1. ^ Principles and Practice of Pharmacology for Anaesthetists By Norton Elwy Williams, Thomas Norman Calvey Published 2001 Blackwell Publishing ISBN 0632056053
  2. ^ Zhu BT (2005). "Mechanistic explanation for the unique pharmacologic properties of receptor partial agonists". Biomed. Pharmacother. 59 (3): 76–89. doi:10.1016/j.biopha.2005.01.010. PMID 15795100. 
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  • This page was last modified on 26 October 2008, at 19:33.

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