CCKBR Antagonist

L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance.

Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent, highly selective and orally active Gastrin/CCK-B antagonist with an IC₅₀ value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC₅₀ of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with K_i values of 0.068, 0.62 and 0.19 nM, respectively.

Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [³H]CCK-8 to the human CCK-2 receptor with a K_i value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.

Pranazepide (FR120480) is a selective cholecystokinin-1 receptor (CCK1-R) antagonist with an IC₅₀ of 0.67 nM against CCK1-R. Pranazepide is applicable for the research of pancreatic diseases.

JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pK_is of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease.

GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with K_i of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder.

Gastrazole (JB95008) is potent and selective CCK2/gastrin receptor antagonist. Gastrazole can decrease the level of gastric acid. Gastrazole inhibits the Gastrin-stimulated growth of pancreatic cancer.

PD 135158 (CAM 1028) is a selective CCK_B receptor antagonist with an IC₅₀ of 2.8 nM against mouse cortex CCK_B. PD 135158 shows anxiolytic activity.

Itriglumide (CR 2945) is an anthranilic acid derivative. Itriglumide is a potent and selective CCKB receptor antagonist, with an IC₅₀ of 2.3 nM. Itriglumide antagonizes the response to gastrin in a dose-dependent manner with an IC₅₀ of 5.9 nM. Itriglumide shows antisecretory and antiulcer activity.

TP-680 is a cholecystokinin receptor antagonist. TP-680 binds 1510 times more strongly to rat pancreatic CCK_A receptors (IC₅₀=1.2 nM) than to rat brain CCK_B receptors (IC₅₀=1812.5 nM). TP-680 can be used in the study of gastrointestinal diseases.

S-0509 is a selective CCKB/gastrin receptor antagonist. S-0509 has a strong anti-secretion effect. S-0509 helps prevent the occurrence of duodenal ulcers.