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Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin.[1] There are two different subtypes CCKA and CCKB which are ~50% homologous:[2] Various cholecystokinin antagonists have been developed and are used in research, although the only drug of this class that has been widely marketed to date is the anti-ulcer drug proglumide.
| Protein | Gene | Tissue distribution | Preferred ligand | Function | Mechanism |
|---|---|---|---|---|---|
| CCKA (CCK1) | CCKAR | primarily gastrointestinal tract, lesser amounts in the CNS | sulfated CCK >> nonsulfated CCK ≈ nonsulfated CCK | stimulation of bicarb secretion, gall bladder emptying and inhibiting gut motility | Gq[3][4] |
| CCKB (CCK2) | CCKBR | primarily CNS, lesser amounts in the gastrointestinal tract | gastrin ≈ CCK (receptor does not discriminate between sulfated and nonsulfated peptides) | regulation of nociception, anxiety, memory and hunger | Gq/G11[4] |
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