- Nomenclature
- cholecystokinin A receptor
- Available assay modes
- Agonist, Inverse agonist, Antagonist, PAM, NAM
- Panels
- à la carte, Oncology, Endocrinology/Metabolism, Psychiatry, Gastrointestinal, Human non-orphan GPCRs
Cholecystokinin receptors
Cholecystokinin receptors are activated by the endogenous peptides cholecystokinin-8 (CCK-8), CCK-33, CCK-58 and gastrin (gastrin-17). There are only two distinct subtypes of CCK receptors, CCK1 and CCK2 receptors [1,2], with some alternatively spliced forms most often identified in neoplastic cells. The CCK receptor subtypes are distinguished by their peptide selectivity, with the CCK1 receptor requiring the carboxyl-terminal heptapeptide-amide that includes a sulfated tyrosine for high affinity and potency, while the CCK2 receptor requires only the carboxyl-terminal tetrapeptide shared by each CCK and gastrin peptides. These receptors have characteristic and distinct distributions, with both present in both the central nervous system and peripheral tissues.References
- Kopin AS, Lee YM, McBride EW, et al. Expression cloning and characterization of the canine parietal cell gastrin receptor. Proc Natl Acad Sci USA 1992;89:3605-9.
- Wank SA, Harkins R, Jensen RT, et al. Purification, molecular cloning, and functional expression of the cholecystokinin receptor from rat pancreas. Proc Natl Acad Sci USA 1992;89:3125-9.
