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Cholecystokinin receptor 2 (CCK2R), also known as the cholecystokinin B receptor or gastrin receptor, is a G protein-coupled receptor (GPCR) with seven transmembrane domains that mediates the physiological actions of both cholecystokinin (CCK) and gastrin peptides. CCK2R is expressed primarily in the gastric mucosa (particularly in acid-secreting parietal cells) and widely in the central nervous system. It regulates key biological processes including gastric acid secretion, appetite, gastrointestinal motility, and cellular proliferation. CCK2R is distinguished from the CCK1R subtype by its similar affinity for CCK and gastrin (including both sulfated and non-sulfated forms), while CCK1R is more selective for sulfated CCK. CCK2R plays a role in a variety of pathological states, including gastrointestinal and neuroendocrine cancers, as well as potential roles in psychiatric and neurological diseases. Multiple small-molecule and peptide agonists and antagonists targeting CCK2R have been developed for research and potential therapeutic use[1][3][4][5][6][7][8].
Antagonism of CCK2R to inhibit gastric acid secretion or modulate tumor growth; Agonism to stimulate acid secretion or GI motility (experimental); Inhibition of signal transduction pathways mediated by gastrin and cholecystokinin[4][5][6]
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