Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin .[ 1] CCKA and CCKB which are ~50% homologous :[ 2] 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]
^ Noble F, Wank SA, Crawley JN , Bradwejn J, Seroogy KB, Hamon M, Roques BP (December 1999). "International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors" . Pharmacological Reviews . 51 (4): 745–781. PMID 10581329 . ^ Dufresne M, Seva C, Fourmy D (July 2006). "Cholecystokinin and gastrin receptors". Physiological Reviews . 86 (3): 805–847. doi :10.1152/physrev.00014.2005 . PMID 16816139 . ^ Wank SA (April 1998). "G protein-coupled receptors in gastrointestinal physiology. I. CCK receptors: an exemplary family". The American Journal of Physiology . 274 (4 Pt 1): G607–G613. doi :10.1152/ajpgi.1998.274.4.g607 . PMID 9575840 . S2CID 27674659 . ^ a b Beinfeld M, Chen Q, Gao F, Liddle RA, Miller LJ, Rehfeld J (2019-09-16). "Cholecystokinin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database" . IUPHAR/BPS Guide to Pharmacology CITE . 2019 (4). doi :10.2218/gtopdb/F15/2019.4 S2CID 203825385 .
