Target intelligence / Profile preview

Cholecystokinin A receptor (CCK1R) (CCK1R)

Target
CCK1R
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Cholecystokinin A receptor (CCK1R) is a G protein-coupled receptor primarily located in the gastrointestinal tract and specific regions of the central nervous system (UniProt P32238). It plays a critical role in regulating digestive processes, including the stimulation of pancreatic enzyme secretion, gallbladder contraction, and the slowing of gastric emptying (IUPHAR/BPS Guide to Pharmacology). Beyond digestion, CCK1R is a key mediator of postprandial satiety, making it a significant target for obesity and metabolic disorder research (PubMed PMID: 25051059). In disease states, dysregulation of CCK1R signaling is associated with gallbladder dysfunction, irritable bowel syndrome, and certain types of cancer, particularly pancreatic adenocarcinoma (NCBI Gene ID: 886). Pharmacological modulation of the receptor includes agonists developed to induce weight loss and antagonists aimed at treating gastrointestinal motility disorders or pain (StatPearls: Physiology, Cholecystokinin). Despite its therapeutic potential, targeting CCK1R presents challenges such as maintaining selectivity over the closely related CCK2 receptor and managing gastrointestinal side effects.

Other names
CCK-A receptorCCKARCholecystokinin receptor type 1Cholecystokinin receptor type ACCK1 receptor
02

Mechanism of action

Agonism of the receptor stimulates satiety and digestive enzyme release, while antagonism is used to inhibit gastrointestinal motility and reduce pain (IUPHAR/BPS Guide to Pharmacology).

03

Biological functions

Signal transductionDigestionSatietyGallbladder contractionPancreatic secretion
04

Disease associations

ObesityDiabetesGastrointestinal disorderCancer
05

Safety considerations

Gastrointestinal distressNauseaPotential for gallstone formationCNS side effects
06

Interacting drugs

Devazepide

5 more in the full profile.

07

Biomarkers

Plasma cholecystokinin levelsGallbladder ejection fraction

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