Target intelligence / Profile preview

Cholecystokinin B Receptor (CCKBR)

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

Overview

The cholecystokinin B receptor (CCKBR) is a G protein-coupled receptor that binds cholecystokinin (CCK) and gastrin. It is primarily found in the central nervous system and gastrointestinal tract. Upon ligand binding, the receptor couples to G proteins, mainly Gq/G11, activating phospholipase C signaling pathways. It plays a role in anxiety, feeding behavior, memory, nociception, gastric acid secretion, and dopamine activity. Altered expression is seen in some cancers and polymorphisms are linked to anxiety and hallucinations.

Other names
CCK-BRCCK2-RCholecystokinin‑2 ReceptorGastrin receptor
02

Mechanism of action

Agonists activate the receptor leading to G protein activation, mainly Gq/G11, which activate phospholipase C signaling pathways leading to intracellular calcium mobilization. Antagonists block the receptor preventing activation by endogenous ligands.

03

Biological functions

Signal transductionRegulation of gastric acid secretionModulation of anxietyModulation of feeding behaviorModulation of memoryModulation of nociception/pain perceptionModulation of dopamine activity
04

Disease associations

CancerAnxiety disordersParkinson's DiseaseAddictionNeuropsychiatric conditions
05

Safety considerations

Potential impact on drug responses related to addictionPotential impact on drug responses related to neuropsychiatric conditions
06

Interacting drugs

Gastrin I

5 more in the full profile.

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