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LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).1 It is selective for CB1 over α1- and α2- adrenergic, D1 and D2 dopamine, benzodiazepine, histamine H1, GABA, serotonin (5-HT), and muscarinic receptors. It reverses the inhibition of forskolin-induced cAMP accumulation induced by arachidonoyl ethanolamide (anandamide; Item No. 90050) in CHO cells and inhibits a stimulatory effect of arachidonoyl ethanolamide on adenylate cyclase induced by application of pertussis toxin (IC50 = 734 nM). LY320135 (1 mg/kg) reverses inhibition of light-induced phase shifts in hamsters induced by the CB1 agonist CP 55,940 (Item No. 90084).2
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1. LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J. Pharmacol. Exp. Ther. 284(1), 291-297 (1998).
2. Cannabinoids and hamster circadian activity rhythms. Brain Res. 1222, 141-148 (2008).