SR 146131 is a potent and selective agonist of the nonpeptide receptor.

SR 146131 is a potent CCK1 agonist on several intracellular events linked to CCK1 receptor activation in various cell types: on [Ca2+]i release and IP1 formation, SR 146131 appears as a full CCK1 receptor agonist in the 3T3-hCCK1 cells, but a partial CCK1receptor agonist on MAPK activation and early gene expression in this cell line. SR 146131 inhibits the binding of [125I]-BH-CCK-8S to CCK1sites on 3T3-hCCK1 cell membranes (IC50: 0.56 ± 0.10 nM). SR 146131 also inhibits the binding of radiolabeled CCK to CCK2sites in CHO-hCCK2 membranes (IC50: 162 ± 27 nM) at much higher concentrations. SR 146131 also acts as a partial agonist in the two neuroblastoma cell lines [1].

SR 146131, when administered orally (p.o.) to mice, completely inhibits gastric and gallbladder emptying, demonstrating efficacy with ED50 values of 66 and 2.7 μg/kg, respectively. At a dose of 10 mg/kg p.o., it notably increases the count of Fos-positive cells within the hypothalamic paraventricular nucleus in rats. Additionally, SR 146131 consistently reduces food intake across various conditions and species, starting at low doses (0.1 mg/kg p.o.) in fasted rats, at 0.3 mg/kg p.o. in nonfasted rats with neuropeptide Y (1–36) induced appetite enhancement, in fasted gerbils, and in marmosets on a restricted diet from doses as low as 3 mg/kg p.o. Moreover, it diminishes locomotor activity in mice at doses beginning from 0.3 mg/kg p.o.