BMS-604992 (EX-1314) free base is a selective, orally active, small-molecule growth hormone secretagogue receptor (GHSR) agonist with high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM), capable of stimulating food intake in rodents.

GHSR:Ki: 2.3 nM, GHSR:0.4 nM (EC50)

BMS-604992 demonstrates high-affinity binding (K i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM) for the ghrelin receptor[1].

BMS-604992 (500 μg/kg; i.p.; 5 minutes) significantly increases gastric emptying compared to vehicle-treated mice[1]. BMS-604992 (1~1000 mg/kg; p.o.; 1 hour) exhibits a dose-linear increase in plasma concentrations and a dose-responsive increase in food intake relative to vehicle-treated controls, with a minimum effective dose of approximately 10 mg/kg[1]. BMS-604992 (300 mg/kg; p.o.; 5~20 minutes) shows a significant difference at the 5-minute time point[1]. BMS-604992 (500 μg/kg; i.p.; 4 hours) increases food intake approximately 2-fold compared to vehicle-treated controls[1]. Animal Models: C57BL/6 mice, SD rat, Male GhrR KO and WT mice.