1: Chem Biodivers. 2007 Aug;4(8):1805-27.

Blocking the cannabinoid receptors: drug candidates and therapeutic promises.

Muccioli GG.

Department of Pharmacology, University of Washington, Seattle, WA 98195, USA.
giulio.muccioli@uclouvain.be

The CB1 and CB2 cannabinoid receptors have been described as two prime sites of
action for endocannabinoids. Both the localization and pharmacology of these two 
G-protein-coupled receptors are well-described, and numerous selective ligands
have been characterized. The physiological effects of Cannabis sativa (cannabis) 
and a throughout study of the endocannabinoid system allowed for the
identification of several pathophysiological conditions--including obesity,
dyslipidemia, addictions, inflammation, and allergies--in which blocking the
cannabinoid receptors might be beneficial. Many CB1 receptor antagonists are now 
in clinical trials, and the results of several studies involving the CB1
antagonist lead compound rimonabant (SR141716A) are now available. This review
describes the pharmacological tools that are currently available and the animal
studies supporting the therapeutic use of cannabinoid receptor antagonists and
inverse agonists. The data available from the clinical trials are also discussed.

PMID: 17712820 [PubMed - indexed for MEDLINE]

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