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.

Targets
Literature
Receptor Data

Cholecystokinin Receptor Target Files

Related Targets

    Literature for Cholecystokinin Receptors

    GPCR

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    Peptides Involved in Appetite Modulation Scientific Review

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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.