PSN632408

GPR119 (previously designated SNORF25) is an orphan G protein-coupled receptor expressed predominantly in the pancreas and gastrointestinal tract in humans and in the brain, pancreas, and gastrointestinal tract in rodents. It mediates a reduction in food intake and body weight gain in rats upon treatment with oleoyl ethanolamide (OEA), an endogenous, potent agonist for PPAR?.{11423,14046} PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively).{14046} Systemic administration of PSN632408 (30 mg/kg intraperitoneally) suppresses food intake, reduces weight gain, and white adipose tissue deposition in rats.{14046} These data suggest that PSN632408 may be useful as a therapeutic agent for the treatment of obesity.