JD-5037

JD-5037 is a peripherally-restricted small molecule inverse agonist of the cannabinoid 1 receptor (CB1). It was developed as an antiobesity drug candidate and is highly selective for CB1 over CB2 receptors. Unlike earlier CB1 antagonists such as rimonabant, JD-5037 does not readily cross the blood-brain barrier and thus avoids central nervous system side effects. Its mechanism involves blockade of peripheral CB1 receptors, leading to decreased leptin expression and secretion, increased leptin clearance by the kidneys, reduced food intake, weight loss, improved glucose and insulin responses in animal models. Additional preclinical studies suggest potential benefits in inflammation and fibrosis models. The compound has also been studied under the name CRB-4001 for metabolic diseases including obesity and non-alcoholic steatohepatitis[2][5][7][9].