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PSB-CB5 is an antagonist of G protein-coupled receptor GPR18 (IC50 = 0.279 µM).1 It is 36-, 36-, and 14-fold selective for GPR18 over GPR55, cannabinoid 1 (CB1), and CB2 receptors, respectively. PSB-CB5 (1 µM) inhibits acrosomal exocytosis induced by the endogenous GPR18 ligand arachidonoyl glycine (NAGly; Item No. 90051) in human spermatozoa.2
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1. Bicyclic imidazole-
2. Characterization of non-