Cholecystokinin receptor (CCKR) (CCKR)

Cholecystokinin receptors (CCKRs) are members of the G protein-coupled receptor (GPCR) superfamily, primarily categorized into two subtypes: CCK1 (formerly CCK-A) and CCK2 (formerly CCK-B) (UniProt P32238, P32239). CCK1 receptors are predominantly found in the gastrointestinal tract, where they mediate gallbladder contraction, pancreatic enzyme secretion, and satiety signaling (StatPearls: Cholecystokinin). In contrast, CCK2 receptors are widely expressed in the central nervous system and the stomach, where they regulate anxiety, memory, and gastric acid secretion (IUPHAR/BPS Guide to Pharmacology). These receptors play significant roles in various physiological processes, including digestion and emotional regulation, making them attractive targets for treating obesity, anxiety, and gastrointestinal disorders (PubMed: PMC2743857). Dysregulation of CCKR signaling is implicated in conditions such as panic disorder and certain types of cancer, particularly pancreatic and gastric malignancies (PubMed: 15608512). Pharmacological interventions include both agonists, aimed at promoting weight loss through satiety, and antagonists, used to manage GI motility and acid-related diseases (PubChem). Despite their therapeutic potential, challenges remain regarding the blood-brain barrier permeability for CNS-targeted ligands and the risk of inducing psychiatric side effects (IUPHAR/BPS Guide to Pharmacology).

Other names

CCK-A receptorCCK-B receptorGastrin receptorCCK1 receptorCCK2 receptorCCK1RCCK2RCholecystokinin A receptorCholecystokinin B receptorCCKARCCKBR

Competitive antagonism of CCK1 or CCK2 receptors to inhibit gastrointestinal motility or gastric acid secretion; agonism to induce satiety and reduce food intake (PubChem, IUPHAR/BPS).