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Target intelligence / Profile preview
Galanin Receptor Type 1 (GALR1)
- Target
- GALR1
- Molecular classification
- G protein-coupled receptor, GPCR, Class A GPCR
01
Overview
Galanin receptor type 1 (GALR1) is a G protein-coupled receptor (GPCR) that binds the neuropeptide galanin. Upon activation by galanin, GALR1 primarily couples to inhibitory G proteins of the Gi/Go family, leading to inhibition of adenylyl cyclase activity and decreased cAMP levels. It is widely expressed in both central and peripheral nervous systems and is involved in various physiological processes, including neurotransmitter release, energy metabolism, pain modulation, and neuroprotection. Several non-peptidic antagonists have been developed, but selectivity among galanin receptor subtypes remains a challenge.
02
Mechanism of action
Inhibition of adenylyl cyclase, activation of GIRK channels, inhibition of calcium channels, activation of MAPK
03
Biological functions
Signal transductionNeuromodulationRegulation of neurotransmitter releaseEnergy metabolism regulationNeuropathic pain modulationEpileptic activity controlSleep homeostasis maintenanceNeuroprotectionCell survivalFeeding behavior controlInsulin release control
04
Disease associations
Neuropathic painEpilepsyNeurodegenerative diseasesFeeding disordersMetabolic disorders
05
Safety considerations
Selectivity challenges among galanin receptor subtypes (GALR1, GALR2, GALR3)
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