Galanin receptor 1 (GALR1)

Galanin receptor 1 is a seven-transmembrane domain G protein-coupled receptor encoded by the GALR1 gene, widely expressed in the brain, spinal cord, heart, and intestine[3][4]. It mediates neuropeptide galanin’s effects—primarily via inhibitory Gi/Go protein signaling—which suppresses cyclic AMP production and regulates neural excitability, mood, pain, and endocrine secretion. GALR1 plays roles both in health (neural modulation, mood, sleep, antinociception) and disease (cancer, epilepsy, depression, inflammation). Its structure has been resolved in complex with galanin and G proteins, revealing a unique extracellular helical ligand-binding mode and distinctive G-protein interface[1][5][6]. The zinc ion inhibits GALR1 function as a negative allosteric modulator[5][6][7].

Other names

GALR1GAL-1GalR1

Ligand binding to GALR1 leads to Gi/Go protein activation, resulting in inhibition of adenylate cyclase and decreased cAMP. Modulation of MAPK signaling via βγ subunit downstream effects. Allosteric modulation (notably by zinc ions as negative regulators).