Figure. Concentration-dependent activation of CCKAR by CCK‐8

Reporter cells were transfected with either the expression plasmid for human cholecystokinin A receptor (CCKAR) or the mock plasmid and treated with various concentrations of CCK‐8. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 17 nM.

cholecystokinin A receptor
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
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.


  1. 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.
  2. 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

Related Receptors

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