Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 28, Issue 11, Pages 567-572Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2007.10.006
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In 2005, the first evidence was obtained that the cannabinoid CB, 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.
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