Cholecystokinin Receptor Data

Receptor Subtype CCK1 Receptors CCK2 Receptors
Transduction Mechanism Gq/11, Gs Gs
Primary Locations Pancreas, gall bladder, intestines, vagus nerve Brain, spinal cord, stomach
Tissue Functions Modulates food intake, pancreatic exocrine secretion and growth, gall bladder contraction, GI motility Modulates anxiety, nociception, neuroleptic activity, gastric acid release, gastric mucosal cell growth and histamine release
Endogenous Ligand Potency CCK octapeptide, sulfated >> gastrin = CCK octapeptide, non-sulfated Gastrin = CCK octapeptide, sulfated = CCK octapeptide, non-sulfated
Selective Agonists A-71623 (2411) Gastrin I (human) (3006)
Selective Antagonists Devazepride (2304)
SR 27897 (2190)
LY 225910 (1018)
YM 022 (1408)
LY 288513 (1524)
CI 988 (2607)
PD 135158 (2608)

References

Wank (1998) G Protein-coupled receptors in gastrointestinal physiology I. CCK receptors: an exemplary family. Am.J.Physiol. 274 G607. Noble et al (1999) International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors. Pharmacol.Rev. 51 745.