Target intelligence / Profile preview

Cholecystokinin 1 receptor (CCK1 receptor)

Target
CCK1 receptor
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

The Cholecystokinin 1 receptor (CCK1 receptor) is a class A G protein-coupled receptor involved in mediating the effects of the peptide hormone cholecystokinin (CCK). It is primarily localized in the pancreas, gall bladder, intestine, and vagus nerve, regulating digestion, pancreatic secretion, gallbladder contraction, and satiety. The receptor also plays a role in CNS pathways mediating dopamine and beta-endorphin release and has recently been associated with neuroprotective effects in diseases like Alzheimer’s and Parkinson’s. CCK1 receptor is a key therapeutic target for obesity and metabolic disorders, with interest in developing safer, more selective agonists and allosteric modulators due to concerns about efficacy and side effects of earlier drugs. Sensitivity to membrane cholesterol may affect drug response in obese individuals.

Other names
Cholecystokinin A receptorCCK1 receptorCCKAR
02

Mechanism of action

Agonists: Stimulate CCK1 receptor to induce satiety, gallbladder contraction, pancreatic secretion; Antagonists: Block receptor activity, useful in modulating GI motility and other conditions; Allosteric modulators: Bind distinct receptor sites to modify response, possibly enabling improved safety/efficacy profiles for obesity and metabolic diseases.

03

Biological functions

Signal transductionRegulation of satiety/appetitePancreatic enzyme secretionSmooth muscle contraction (gallbladder, stomach)Dopamine and beta-endorphin releaseNeuroprotectionModulation of glucose levelsSuppression of inflammationIntestinal protection
04

Disease associations

ObesityMetabolic disordersNeurodegenerative diseases (Alzheimer’s, Parkinson’s)InflammationDigestive diseases
05

Safety considerations

Side effects from full agonists: Lack of effectiveness vs. dieting, GI upset, tolerance, dependencePotential for toxicity with high potency/duration drugsCholesterol sensitivity: Impaired receptor signaling in obese patients, leading to possible drug refractoriness
06

Interacting drugs

Cholecystokinin

11 more in the full profile.

07

Biomarkers

Cholecystokinin peptide levels (for receptor activation/satiety response)Brain-derived neurotrophic factor (BDNF) (in neuroprotection contexts)Obesity/metabolic syndrome markers (clinical research/efficacy endpoints)

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