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(Redirected from Partial Agonist)
Agonist drug having partial efficacy at a receptor
Relationship between percentage activity and concentration of full agonists and partial agonists
In pharmacology, partial agonists are drugs that bind to 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. Clinically, partial agonists can be used to 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.
Calvey N, Williams N (2009). "Partial agonists". Principles and Practice of Pharmacology for Anaesthetists. John Wiley & Sons. p. 62. ISBN978-1-4051-9484-6.
Zhu BT (April 2005). "Mechanistic explanation for the unique pharmacologic properties of receptor partial agonists". Biomedicine & Pharmacotherapy. 59 (3): 76–89. doi:10.1016/j.biopha.2005.01.010. PMID15795100.
