YIL 781

An antagonist of GHS-Ra (Ki = 0.017 µM), is selective for GHS-Ra over the motilin receptor (Ki = 6 µM) and a panel of 30 receptors and enzymes (Kis = > 10 µM), prevents ghrelin-induced decreases in insulin secretion in glucose-stimulated isolated rat pancreatic islets at concentration of 1 µM, increases plasma insulin levels and decreases blood glucose levels in an intraperitoneal glucose tolerance test in rats at doses of 0.3 or 10 mg/kg, respectively, inhibits cocaine-induced hyperlocomotion in mice at 10 and 20 mg/kg. SMILES: FC1=CC=C(OC2=CC=C(N=C(C)N(C[C@H]3CCCN(C(C)C)C3)C4=O)C4=C2)C=C1. InChi Code: InChI=1S/C24H28FN3O2/c1-16(2)27-12-4-5-18(14-27)15-28-17(3)26-23-11-10-21(13-22(23)24(28)29)30-20-8-6-19(25)7-9-20/h6-11,13,16,18H,4-5,12,14-15H2,1-3H3/t18-/m0/s1. InChi Key: FRKXOBMDEXCHHD-SFHVURJKSA-N