Cholecystokinin receptors
Overview
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.
Excerpt from IUPHAR/BPS Guide to Pharmacology Filters Sort resultsReset ApplyFilters Sort resultsReset Apply
Species Receptor Family Assays Human AvailableAssay modes:Agonist⋅Inverse agonist⋅Antagonist⋅PAM⋅NAMPanels:Human non-orphan GPCRs⋅Oncology⋅Endocrinology/Metabolism⋅Psychiatry⋅Gastrointestinal⋅à la carte Human AvailableAssay modes:Agonist⋅Inverse agonist⋅Antagonist⋅PAM⋅NAMPanels:Human non-orphan GPCRs⋅Oncology⋅Endocrinology/Metabolism⋅Psychiatry⋅Neurology⋅Gastrointestinal⋅à la carte Mouse AvailableAssay modes:Agonist⋅Inverse agonist⋅Antagonist⋅PAM⋅NAMPanels:Mouse non-orphan GPCRs⋅à la carte Mouse AvailableAssay modes:Agonist⋅Inverse agonist⋅Antagonist⋅PAM⋅NAMPanels:Mouse non-orphan GPCRs⋅à la cartePAGE TOP