JD5037

JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM). It displays >700-fold selectivity for CB1 over CB2, >1,000-fold selectivity over a panel of 70 receptors, transporters, and ion channels, and low blood-brain barrier penetrance. JD5037 is orally bioavailable and reduces food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obese mice. JD5037 reverses hyperphagia, reduces body weight, and improves metabolic parameters in Magel2-null mice, a model of Prader-Willi syndrome.