Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies |
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| Authors: | Lavey Brian J Kozlowski Joseph A Hipkin R William Gonsiorek Waldemar Lundell Daniel J Piwinski John J Narula Satwant Lunn Charles A |
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| Institution: | Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-1-1545, Kenilworth, NJ 07033-0539, USA. brian.lavey@spcorp.com |
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| Abstract: | 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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