cck-b

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.

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

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.

GV-150013X ((S)-1-(1-(adamantan-1-ylmethyl)-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl)-3-phenylurea) is a potent CCKB antiagonist, pKi= 9.02.

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

Sograzepide (Netazepide) is an orally active, selective and highly potent gastrin/CCK-B antagonist that inhibits gastrin/CCK-A activity and pappalysin 2 expression in type 1 gastric neuroendocrine tumors, and can induce regression of type 1 gastric neuroendocrine tumors.

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.

Selective CCK2 receptor antagonist

PD 135158 is a CCK2 receptor antagonist.

PD-149164 is an agonist of the CCK-A receptor.

TP-680 is a antagonist of cholecystokininA receptor.

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.

CCK2 (CCK-B) receptor antagonist

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.

BC 197 is a selective CCK-B agonist.

Snf 8815 is an antagonist of cholecystokinin-B (CCK-B).

A-57696 is a cholecystokinin antagonist with selective for cortical CCK-B receptors (IC50 = 25 nM).

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).

L-740093 is a specific antagonist of CCK-B receptor.

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

L-365260 hemihydrate is a selective, orally active non-peptide gastrin and brain cholecystokinin receptor (CCK-B) antagonist, demonstrating competitive interaction with guinea pig stomach gastrin and brain CCK receptors and exhibiting inhibition constants (Kis) of 1.9 nM and 2.0 nM, respectively.