Dexloxiglumide is a cholecystokinin (CCK) receptor antagonist and is the single (R) isomer of loxiglumide .1,2 It selectively binds to the CCK1 receptor over CCK2 in CHO cells expressing the rat receptors (Kis = 0.0234 and 5.88 ?M, respectively).1 Dexloxiglumide (20 ?mol/kg) inhibits guinea pig gallbladder contractions induced by the CCK agonist CCK octapeptide (sulfated) . It reduces CCK-8-induced gastric emptying in rats (ID50 = 1.14 mg/kg).2
1.Morton, M.F., Barrett, T.D., Yan, W., et al.3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: In vitro and in vivo pharmacological comparison with dexloxiglumideJ. Pharmacol. Exp. Ther.323(2)562-569(2007) 2.Scarpignato, C., Kisfalvi, I., D'Amato, M., et al.Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: Evaluation of their receptor selectivity in vivoAliment. Pharmacol. Ther.10(3)411-419(1996)