cck 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.

Proglumide (Binoside) is a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

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

Pentagastrin (ICI-50123) is a synthetic polypeptide that mimics the effects of gastrin when administered parenterally, influencing the secretion and synthesis of salivary proteins.

Sincalide (CCK-8) is a cholecystokinetic drug administered by injection to aid in diagnosing disorders of the gallbladder and pancreas. It is the 8-amino acid C-terminal fragment of cholecystokinin.

Nastorazepide (Z-360) is a selective, orally available antagonist of the gastrin/cholecystokinin 2 (CCK-2) receptor with potential antineoplastic activity.

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).

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.

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.

Itriglumide (CR-2945) is a cholecystokinin (CCK)-2 receptor antagonist with antisecretory and antiulcerogenic properties.

N-Cbz-DL-tryptophan is a cholecystokinin receptor antagonist, abolished the response of the isolated heart to CCK-8.

Tarazepide is a potent and specific antagonist of the CCK-A receptor.

Ceruletide Ammonium acetate (FI-6934 Ammonium acetate) is a cholecystokinin (CCK) receptor agonist. Ceruletide Ammonium acetate is a safe and effective cholecystokinetic agent and small bowel and exocrine pancreatic stimulant.

Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist and the pharmacologically active enantiomer of Loxiglumide, effectively inhibiting smooth muscle contractions induced by cholecystokinin-octapeptide (CCK-8), while displaying moderate, polarized, concentration-dependent, and pH-dependent Caco-2 permeability and increasing uptake of the MRP1 substrate fluorescein. Dexloxiglumide supports the mechanistic studies of gastrointestinal disorders and tumor-related smooth muscle and transporter biology.

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.

Nastorazepide (Z-360) hemicalcium is a selective, orally-administered 1,5-benzodiazepine derivative that functions as a receptor antagonist for gastrin/cholecystokinin 2 (CCK-2), exhibiting potential antitumor activity.

Lorglumide (CR-1409) is a potent cholecystokinin (CCK) receptor antagonist. It is employed in studies involving pancreatic secretion and growth.

CCK2 (CCK-B) receptor antagonist

L-365260 is an orally available, selective and potent nonpeptide gastrin and cerebral cholecystokinin receptor (CCK-B) antagonist.L-365260 inhibits CCK-8S-induced increase in [Ca2+]i, blocks stress-induced hypersensitivity in viscera, and blocks the anti-exploratory effect of CCK-4.L-365260 has been used in the study of neurological Ojibwa and endocrine diseases.

Cholecystokinin (27-32)-amide is a CCK receptor antagonist.

Jmv 332 is a cyclic analog of the C-terminal hexapeptide of CCK. It is a CCK/gastrin receptor agonist.

CI-1015 is a CCK-B receptor antagonist with oral activity.

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).