Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies

Brian J Lavey, Joseph A Kozlowski, R William Hipkin, Waldemar Gonsiorek, Daniel J Lundell, John J Piwinski, Satwant Narula, Charles A Lunn
Bioorganic & Medicinal Chemistry Letters 2005 February 1, 15 (3): 783-6
A novel class of cannabinoid CB2 receptor ligands is described. These triaryl bis-sulfones are nanomolar inhibitors of the CB2 receptor and show high selectivity over the cannabinoid CB1 receptor. One example of this new class decreases ligand-induced GTPgammaS binding to recombinant CB2 cell membranes, identifying the compound as a CB2-selective inverse agonist.

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