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Bioorg Med Chem Lett. 2005 Feb 1;15(3):783-6.

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

Author information

1
Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-1-1545, Kenilworth, NJ 07033-0539, USA. brian.lavey@spcorp.com

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.

PMID:
15664857
DOI:
10.1016/j.bmcl.2004.11.007
[Indexed for MEDLINE]

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