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The Cholecystokinin 1 receptor (CCK1 receptor) is a class A G protein-coupled receptor involved in mediating the effects of the peptide hormone cholecystokinin (CCK). It is primarily localized in the pancreas, gall bladder, intestine, and vagus nerve, regulating digestion, pancreatic secretion, gallbladder contraction, and satiety. The receptor also plays a role in CNS pathways mediating dopamine and beta-endorphin release and has recently been associated with neuroprotective effects in diseases like Alzheimer’s and Parkinson’s. CCK1 receptor is a key therapeutic target for obesity and metabolic disorders, with interest in developing safer, more selective agonists and allosteric modulators due to concerns about efficacy and side effects of earlier drugs. Sensitivity to membrane cholesterol may affect drug response in obese individuals.
Agonists: Stimulate CCK1 receptor to induce satiety, gallbladder contraction, pancreatic secretion; Antagonists: Block receptor activity, useful in modulating GI motility and other conditions; Allosteric modulators: Bind distinct receptor sites to modify response, possibly enabling improved safety/efficacy profiles for obesity and metabolic diseases.
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