UNIT 1.1 Receptors as Drug Targets

  1. Michael Williams,
  2. Rita Raddatz

Published Online: 1 APR 2006

DOI: 10.1002/0471141755.ph0101s32

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Williams, M. and Raddatz, R. 2006. Receptors as Drug Targets. Current Protocols in Pharmacology. 32:1.1:1.1.1–1.1.18.

Author Information

  1. Worldwide Discovery Research Cephalon, Inc., West Chester, Pennsylvania

Publication History

  1. Published Online: 1 APR 2006
  2. Published Print: MAR 2006


Receptors, located on both the cell surface and within the cell, are the molecular targets through which drugs produce their beneficial effects in various disease states. Receptors were initially conceptualized at the beginning of the 20th century by the parallel efforts of Ehrlich and Langley. The concepts of the receptor and receptor theory, based on the Law of Mass Action, have undergone continuous refinement as they have been characterized in terms of their molecular structure, association with ancillary proteins (e.g., G proteins, arrestins, RAMPs), and functional characteristics in normal and diseased tissues. The concepts describing ligand interactions with receptors have also been refined from the simple binary concept of competitive agonists and antagonists to partial agonists, allosteric modulators and inverse agonists. Concepts such as receptor constitutive activity, internalization and dimerization add additional complexity to the role of receptors in tissue function and in precisely characterizing their role in homeostasis and disease.


  • agonist;
  • antagonist allosteric modulator;
  • G protein-coupled receptor;
  • heterotrimeric G protein;
  • ion channels;
  • ligand;
  • new chemical entity (NCE);
  • orphan receptor;
  • structure activity relationship (SAR)