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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.
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
|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)|
SR 27897 (2190)
LY 225910 (1018)
YM 022 (1408)
LY 288513 (1524)
CI 988 (2607)
PD 135158 (2608)
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.