cholecystokinin 1 receptor

GI 181771 is an agonist of the cholecystokinin 1 receptor. GI 181771 can be used in studies about obesity.

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

Ceruletide is a decapeptide that serves as a safe and effective cholecystokinin receptor agonist, exerting a direct spasmogenic effect on the gallbladder muscle and bile ducts, and is commonly used to establish pancreatitis models.

CCK-A receptor inhibitor 1 is a potent cholecystokinin A (CCK-A) receptor inhibitor (IC50: 340 nM) and can be used to study digestive system-related diseases.

CCK-B Receptor Antagonist 1 is a cholecystokinin B (CCK-B) receptor agonist and has the potential of reducing the secretion of gastric acid.

Devazepide is a competitive, selective, orally available non-peptide CCK1 (cholecystokinin 1) receptor antagonist that inhibits bladder cancer cell proliferation and migration while inducing apoptosis and cell cycle arrest.

ZP3022 is a dual agonist targeting the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor. It selectively enhances cAMP accumulation or ERK phosphorylation in HEK293 cells with GLP-1R or CCK2 receptor expression, compared to ERK phosphorylation in cells with the CCK1 receptor (EC50s: 0.02, 10.3, and >1,000 nM for human receptors, respectively). At 40 nM, ZP3022 promotes proliferation of rat neonatal β-cells in vitro. It also boosts glucose-induced insulin secretion (GSIS) in rat pancreatic islets at 10 and 100 nM concentrations and decreases body weight in rats at 40 nmol/kg doses twice daily. Administered at 100 nmol/kg daily, ZP3022 enhances β-cell and total pancreatic mass and improves glucose tolerance in db/db mice, while reducing food intake but not body weight in these mice.

Loxiglumide (CR-1505) is an antagonist of cholecystokinin (CCK-1) receptor.

JNJ-17156516 is a potent, and selective cholecystokinin 1 receptor antagonist.

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.

CCKBRagonist-1 (Compound 3r1) is a selective agonist for the cholecystokinin B receptor (CCKBR) that preferentially activates the Gq protein, with an EC50 of 35 pM. It significantly enhances neuronal survival at an EC50 of 37 pM. CCKBRagonist-1 improves cognitive decline in mice by upregulating α-secretase (ADAM10) and the calcium signaling molecule PLCB4, reduces the number of amyloid β (Aβ) plaques, and promotes long-term potentiation (LTP). This compound is useful for Alzheimer's disease research.