A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.ObesityPhase 3 Discontinued

Anandamide, an immune modulator, acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55) in the central nervous system.

AM6545 is a selective and potent peripheral restricted cannabinoid receptor 1 (CB1) antagonist that inhibits the CB2 receptor, ameliorates hypometabolic obesity and improves adipokine secretion in monosodium glutamate-induced obese mice, and may be useful in the study of obesity and diabetes.