Cholecystokinin receptor type 1 (CCK1R)

Cholecystokinin receptor type 1 (CCK1R) is a member of the class A G protein-coupled receptor (GPCR) family that primarily couples to Gq/11 proteins. It is distinguished by seven transmembrane helices and signature motifs characteristic of class A GPCRs. CCK1R is highly expressed in peripheral tissues, including the pancreas, gallbladder, stomach, and vagal afferent nerves, and mediates the actions of the peptide hormone cholecystokinin (CCK). These actions include stimulating gallbladder contraction, pancreatic enzyme secretion, relaxing the sphincter of Oddi, delaying gastric emptying, and promoting satiety by reducing food intake[1][2][4][7]. CCK1R is a validated therapeutic target for metabolic and gastrointestinal diseases, especially obesity, but drug development has been challenging due to side effects and limited efficacy. Selective antagonists and agonists have been developed, with ongoing research in allosteric modulation and biased agonism to improve therapeutic profiles[3][6][9]. The receptor’s function can be modulated by membrane cholesterol, which is relevant for patient populations with metabolic syndrome or obesity[9].

Other names

CCK1 receptorCCK-A receptorCholecystokinin A receptorCCKAR

Antagonists block endogenous peptide (CCK) action at the receptor to modulate appetite and gastrointestinal functions. Agonists mimic CCK for satiety/weight loss. Allosteric modulation alters receptor response for increased selectivity or fewer side effects[3][6]