Cholecystokinin Receptors
Cholecystokinin (CCK) is a neuropeptide and gut hormone that regulates pancreatic enzyme secretion and gastrointestinal motility, and acts as a satiety signal. It is released simultaneously from intestinal cells and neurons in response to a meal. The precursor molecule prepro-CCK can be cleaved to generate a variety of biologically active forms of CCK including CCK-33, CCK-8 (CCK octapeptide), CCK-39 and CCK-58. Two CCK receptor subtypes, CCK1 and CCK2, mediate the physiological actions of CCK and the related peptide gastrin. The CCK1 receptor has a high affinity for sulfated CCK analogs, whereas the CCK2 receptor has similar affinity for sulfated and non-sulfated forms.
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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.