Current Knowledge on the Antagonists and Inverse Agonists of Cannabinoid Receptors
G. G. Muccioli and D. M. Lambert
Affiliation: 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.
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: cannabinoid, antagonism, inverse agonism, rimonabant, sr, slv
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