Target intelligence / Profile preview

Galanin receptor 3 (GALR3) (GALR3)

Target
GALR3
Molecular classification
G protein-coupled receptor, Class A GPCR, Receptor
01

Overview

Galanin receptor 3 (GALR3) is a Class A G protein-coupled receptor (GPCR) that serves as a key mediator for the neuropeptide galanin and the peptide spexin. It is primarily expressed in the central nervous system, particularly in the hypothalamus, amygdala, and hippocampus, as well as in the retina and peripheral vasculature. GALR3 signaling predominantly occurs via the Gi/o-protein pathway, leading to the inhibition of adenylyl cyclase and the modulation of potassium channels. This receptor is a significant therapeutic target for neuropsychiatric conditions, with selective antagonists demonstrating potential in preclinical models for treating anxiety, depression, and alcohol use disorders. Recent research also suggests a role for GALR3 in ocular health, specifically in protecting against inflammation and oxidative stress in retinal degenerative diseases like retinitis pigmentosa. While several high-affinity research tools such as SNAP-37889 exist, no GALR3-targeted drugs are currently approved for clinical use.

Other names
Galanin receptor type 3GAL3-RGALR-3GALNR3GAL3 receptor
02

Mechanism of action

Competitive antagonism of the GALR3 receptor to block Gi/o-mediated signaling pathways, which is associated with anxiolytic and anti-addictive effects; or agonism via endogenous peptides and synthetic ligands to modulate neurotransmission and metabolic homeostasis.

03

Biological functions

Signal transductionNeurotransmissionMood regulationFeeding behaviorRegulation of alcohol consumptionInflammatory response modulationNociception
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Disease associations

AnxietyDepressionAlcoholismRetinal degenerationRetinitis pigmentosaNeuropathic painDiabetes
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Safety considerations

Blood-brain barrier permeability of ligands for CNS targetsSelectivity over GALR1 and GALR2 subtypesPotential for behavioral or mood-related side effectsInteractions with broader neuropeptide regulatory networks
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Interacting drugs

SNAP-37889

5 more in the full profile.

07

Biomarkers

GALR3 mRNA expression levelsGalanin peptide levels in CSF or serumRetinal thickness and morphologyElectroretinogram (ERG) response

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