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Current Knowledge on the Antagonists and Inverse Agonists of Cannabinoid Receptors

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Abstract:

Ten years elapsed since the discovery by Sanofi of SR141716A the first selective CB1 cannabinoid receptor antagonist. Shortly after, Sanofi also reported the synthesis of the first selective CB2 cannabinoid receptor antagonist, SR144528. Since these two milestones in the cannabinoid field, many other compounds, more or less related to the Sanofi compounds, or based on a completely different scaffold appeared. Several of these compounds are currently involved in clinical trials for diseases such as obesity, nicotine and alcohol addictions, or allergies. Further, the cannabinoid receptors knock-out mice production strengthened the hypothesis of the existence of several other “cannabinoid” receptors for which the first antagonists begin to appear. The large amount of patents taken by many different pharmaceutical companies prove, if necessary, the great therapeutic potential expected for the cannabinoid receptors antagonists.

Keywords: antagonism; cannabinoid; inverse agonism; rimonabant; slv; sr

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867054020891

Affiliations: Unite de Chimie pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Faculte de Medecine, Universite catholique de Louvain, Avenue E. Mounier, 73, UCL-CMFA 7340, B-1200 Bruxelles, Belgium.

Publication date: June 1, 2005

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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