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.
CE-326597 is a potent and selective CCK1R agonist. The type 1 cholecystokinin receptor (CCK1R) has multiple physiologic roles relating to nutrient homeostasis,including mediation of postcibal satiety. The type 1 cholecystokinin (CCK) receptor (CCK1R) is a key mediator of postcibal satiety and a potential target for drugs that may be useful to prevent and/or treat obesity.
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
Devazepide is a competitive and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor (IC50s: 81 pM, 45 pM, and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCKreceptors, respectively).
Broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. In