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

Trends Pharmacol Sci. 1995 Jun;16(6):188-92. doi: 10.1016/s0165-6147(00)89020-3.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Receptors, Drug / agonists*
  • Receptors, Drug / chemistry


  • Receptors, Drug