Allosterism and cannabinoid CB(1) receptors: the shape of things to come

Trends Pharmacol Sci. 2007 Nov;28(11):567-72. doi: 10.1016/


In 2005, the first evidence was obtained that the cannabinoid CB(1) receptor contains an allosteric binding site. The site can be recognized by synthetic small molecules, which display a markedly divergent effect on orthosteric ligand affinity versus efficacy; these small molecules are allosteric enhancers of agonist binding affinity and allosteric inhibitors of agonist signalling efficacy. Allosteric modulation heralds a new approach to the manipulation of the endocannabinoid system for therapeutic benefit; it promises to augment the existing portfolio of selective direct agonists, competitive antagonists and enzyme inhibitors.

Publication types

  • Review

MeSH terms

  • Allosteric Regulation / drug effects
  • Animals
  • Humans
  • Ligands*
  • Models, Biological
  • Molecular Structure
  • Receptor, Cannabinoid, CB1 / agonists*
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors


  • Ligands
  • Receptor, Cannabinoid, CB1