Principles: receptor theory in pharmacology

Trends Pharmacol Sci. 2004 Apr;25(4):186-92. doi: 10.1016/


Pharmacological receptor theory is discussed with special reference to advances made during the past 25 years. Thus, the operational model has supplanted analysis of drug-receptor interaction in functional systems whereas the extended ternary complex model is used routinely to simulate quantitatively G-protein-coupled receptor (GPCR) behavior. Six new behaviors for GPCRs, centered on spontaneous production of receptor active states, ligand-selective receptor active states, oligomerization with other proteins (receptor and non-receptor) and allosteric mechanisms, have been characterized and each holds the potential for new drug discovery for therapeutic benefit.

Publication types

  • Review

MeSH terms

  • Humans
  • Models, Biological*
  • Pharmacology / trends*
  • Receptors, G-Protein-Coupled* / drug effects
  • Receptors, G-Protein-Coupled* / physiology


  • Receptors, G-Protein-Coupled