Biochem/physiol Actions
PSN-375963 is a GPR119 partial agonist. GPR119 is an orphan GPCR, expressed predominantly in pancreas and GI tract, that has been characterized. Its endogenous ligands are oleoylethanolamide (OEA) and oleoyl-lysophosphatidylcholine, lipid signaling molecules that regulate food intake and body weight. OEA decreases food intake, so GPR119 agonists are potential therapies for obesity. Initial studies showed that PSN-375963 has similar potency and partial efficacy compared to OEA. Further studies revealed that although OEA and PSN-375963 are GPR119 agonists, they have divergent effects on insulin secretion, calcium signaling, and cAMP production.