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).
Proglumide hemicalcium is a antagonist of nonpeptide and orally active cholecystokinin (CCK)-A/B receptors, has antiepileptic and antioxidant activities.
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).
Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gastrin (cholecystokinin type B (CCK-B)) receptor antagonists may help to elucidate the physiological role o
DA-3934 has a high affinity for gastrin/CCK-B receptors and high selectivity over CCK-A receptors. DA-3934 and its methyl ester derivative inhibited pentagastrin-induced gastric acid secretion in rats in a dose-dependent manner.