UNIT 1.1 Receptors as Drug Targets

  1. Michael Williams

Published Online: 1 MAY 2001

DOI: 10.1002/0471141755.ph0101s00

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Williams, M. 2001. Receptors as Drug Targets. Current Protocols in Pharmacology. 1:1.1.

Author Information

  1. Abbott Laboratories, Abbott Park, Illinois

Publication History

  1. Published Online: 1 MAY 2001
  2. Published Print: MAR 1998

This is not the most recent version of the article. View current version (1 APR 2006)


This overview introduces the basic terminology and theory of receptor-ligand interactions. Receptors are envisaged as cell surface recognition sites for endogenous hormones, neurotransmitters, and neuromodulators. Receptor selectivity, binding saturability and reversibility, and functionality are discussed in this unit, with special emphasis placed on receptors being targets for drug development. The term Receptor is now used in a broad sense to describe any recognition site for a compound, the latter being defined as an exogenous chemical or biological substance that acts through a binding site or receptor in tissues. Thus, enzymes, uptake sites, ligand-binding proteins, voltage-gated ion channels, and intracellular targets are also envisaged as receptors. The use of recombinant receptor systems, receptor mutations and chimeras and allosteric ligands are also described in the setting of drug discovery and development.