1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Cholecystokinin Receptor
  4. CCKBR Isoform
  5. CCKBR Antagonist

CCKBR Antagonist

CCKBR Antagonists (6):

Cat. No. Product Name Effect Purity
  • HY-106840
    Antagonist 99.93%
    L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis 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.
  • HY-19445
    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.
  • HY-155205
    GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with Ki of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder.
  • HY-106347
    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.
  • HY-129810
    PD 135158
    PD 135158 (CAM 1028) is a selective CCKB receptor antagonist with an IC50 of 2.8 nM against mouse cortex CCKB. PD 135158 shows anxiolytic activity.
  • HY-111313
    JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis 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.