Target intelligence / Profile preview

Galanin receptor 3 (GALR3)

Target
GALR3
Molecular classification
G protein-coupled receptor, Receptor, Transmembrane protein
01

Overview

Galanin receptor 3 is a 7-transmembrane domain G protein-coupled receptor encoded by the GALR3 gene. It is part of the galanin receptor family, including GALR1 and GALR2, which binds the neuropeptide galanin and spexin. GalR3 is primarily expressed in the hypothalamus, though reports suggest wider distribution in both central and peripheral tissues. It couples mainly to the inhibitory Gi/o pathway, downregulating adenylyl cyclase activity and reducing intracellular cAMP. Biological roles include regulation of energy metabolism, nociception, mood, sleep, and hormone release. Selective ligands remain limited, but GalR3-selective antagonists are under investigation for neuropsychiatric and pain disorders.

Other names
GALR3Galanin receptor type 3GalR3
02

Mechanism of action

Antagonists: block GalR3-mediated Gi/o signaling, potentially anxiolytic and antidepressant effects. Agonists: stimulate Gi/o signaling leading to inhibition of adenylyl cyclase, reduced cAMP, and downstream cellular effects.

03

Biological functions

Signal transductionNeuromodulationRegulation of energy metabolismRegulation of hormone secretionInfluences pain perceptionRegulation of sleep homeostasisCognitive function
04

Disease associations

Neuropathic painEpilepsySleep disordersDepression and mood disordersMetabolic disordersOther neuropsychiatric and neurodegenerative disorders
05

Safety considerations

Limited understanding of tissue distribution and subtype specificity may introduce off-target effects.Central nervous system effects, potential mood alteration, and seizure threshold modulation are concerns for therapeutic development.
06

Interacting drugs

SNAP-37889 (GalR3 selective antagonist)

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