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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Literature (1)
Receptor Data

Cholecystokinin Receptor Target Files

Related Targets

    Literature for Cholecystokinin Receptors

    Tocris offers the following scientific literature for Cholecystokinin Receptors to showcase our products. We invite you to request* your copy today!

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    Peptides Involved in Appetite Modulation Scientific Review

    Peptides Involved in Appetite Modulation Scientific Review

    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.

    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)


    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.