Principles: receptor theory in pharmacology.

Assay Development Compound Profiling, GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA. Terry.P.Kenakin@gsk.com

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.

PMID: 15063082 [PubMed - indexed for MEDLINE]