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.

Receptor Subtype	CCK₁ Receptors	CCK₂ Receptors

Transduction Mechanism	G_q/11, G_s	G_s
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)

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