CCK-B Receptor Antagonist 2 is a potent and orally active antagonist of Gastrin/CCK-B (IC50: 0.43 nM). It also inhibits gastrin/CCK-A activity (IC50: 1.82 μM).
YM022 is a highly effective and selective gastrin/cholecystokinin (CCK)-B receptor antagonist. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively.
L-736380 is a CCK-B receptor antagonist. L-736,380 dose-dependently inhibited gastric acid secretion in anesthetized rats (ID(50), 0.064 mg/kg) and ex vivo binding of [(125)I]CCK-8S in BKTO mice brain membranes (ED(50), 1.7 mg/kg).