PSN375963

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} PSN375963 is a potent and selective agonist of GPR119 that shows similar potency to oleoyl ethanolamide (OEA) at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 8.4 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively).{14046} These data suggest that PSN375963 may be useful as a therapeutic agent for the treatment of obesity.