Description
A CB1 receptor antagonist; binds to CB1 receptors in rat forebrain membrane preparations (Ki = 7.5 nM); selective over CB2 receptors (Ki = 2,290 nM for mouse spleen membrane preparations); inhibits CP 55,940-induced GTPγS binding in HEK293 cells expressing human CB1 receptors (EC50 = 8 nM); decreases immobility time in the forced swim test in wild-type but not CB1 receptor-deficient mice at 10 mg/kg; reduces fasting-induced food intake and body weight gain in mice at 30 mg/kg; induces GTPγS binding in HEK293 cells expressing the orphan receptor GPR55 (EC50 = 39 nM); potentiates GABA-induced GABAA receptor currents (EC50 = 0.4 µM); prevents TGF-β1-induced EMT, inhibits SMAD2/3 and p38 MAPK activation, and reduces the expression of EMT-related transcription factors in HK-2 renal tubule epithelial cells; induces cell cycle arrest at the G2/M phase and apoptosis in A375 human melanoma cells