AM6545

Peripherally-restricted cannabinoid receptor 1 (CB₁) selective antagonists have the potential to inhibit food intake while also escaping centrally-mediated neuropsychiatric side effects. AM6545 is a novel CB₁ selective neutral antagonist with low CNS penetration, exhibiting K_i values of 1.7 and 523 nM for CB₁ and CB₂ receptors, respectively.¹ It reduces food intake and food-reinforced behavior, such as time spent feeding, in a dose-dependent manner, resulting in decreased body weight.^1,2 AM6545 produces improvements in glucose homeostasis, fatty liver, and plasma lipid profiles in mice with diet-induced obesity.³ It does not affect behavior responses that are associated with activation of CB₁ receptors in the brain.³

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1. Cluny, N.L., Vemuri, V.K., Chambers, A.P., et al. A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents. Br. J. Pharmacol. 161(3), 629-642 (2010).

2. Randall, P.A., Vemuri, V.K., Segovia, K.N., et al. The novel cannabinoid CB₁ antagonist AM6545 suppresses food intake and food-reinforced behavior. Pharmacol. Biochem. Behav. 97(1), 179-184 (2010).

3. Tam, J., Vemuri, V.K., Liu, J., et al. Peripheral CB₁ cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity. J. Clin. Invest. 120(8), 2953-2966 (2010).