[Type B (gastrin) receptors of the cholecystokinin (CCK) family are found principally in the CNS and the gastrointestinal tract. In the CNS, they regulate anxiety, arousal, neuroleptic activity, and opiate-induced analgesia. Outside the CNS, they regulate gastric acid secretion and may play a role in gastrointestinal motility and growth of normal and neoplastic gastrointestinal tissue. Cholecystokinin B Receptor (CCKBR), encoded by the CCKBR gene, is a G protein-coupled receptor for gastrin and cholecystokinin. It activates a second messenger system involving phosphatidylinositol turnover and intracellular calcium mobilization. CCKBR can selectively be blocked by nonpeptide benzodiazepine-based antagonists. A single amino acid, valine-319, is critical in determining the binding affinity for these nonpeptide antagonists. Variability in the aliphatic side chain of the amino acid in position 319 confers antagonist specificity. (NCI) ( NCI )]
UMLS (NCI) C0248266 - Amino Acid, Peptide, or Protein
- Receptor
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