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Trends Pharmacol Sci. 1995 Jun;16(6):188-92.

Agonist-receptor efficacy. I: Mechanisms of efficacy and receptor promiscuity.

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Department of Cellular Biochemistry, Glaxo Research Institute, Research Triangle Park, NC 27709, USA.


The description of drug effects on receptor proteins is based on models and equations used to describe mass-action kinetics of molecules and inert surfaces. These models provide an adequate description of drug affinity, that is, how well a molecule binds to a receptor protein, but the way in which ligands change receptor populations to impart signals to cells remains to be determined. In the first of two articles, Terry Kenakin discusses a basic question in receptor pharmacology, namely the nature of ligand efficacy.

[Indexed for MEDLINE]

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