Galanin receptor

The galanin receptor is a G protein-coupled receptor, or metabotropic receptor which binds galanin.^[1]

galanin receptor 1
Identifiers
Symbol	GALR1
Alt. symbols	GALNR1, GALNR
NCBI gene	2587
HGNC	4132
OMIM	600377
RefSeq	NM_001480
UniProt	P47211
Other data
Locus	Chr. 18 q23
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galanin receptor 2
Identifiers
Symbol	GALR2
NCBI gene	8811
HGNC	4133
OMIM	603691
RefSeq	NM_003857
UniProt	O43603
Other data
Locus	Chr. 17 q25.3
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galanin receptor 3
Identifiers
Symbol	GALR3
NCBI gene	8484
HGNC	4134
OMIM	603692
RefSeq	NM_003614
UniProt	O60755
Other data
Locus	Chr. 22 q12.2-13.1
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Galanin receptors can be found throughout the peripheral and central nervous systems and the endocrine system. So far three subtypes are known to exist: GAL-R1, GAL-R2, and GAL-R3.^[2] The specific function of each subtype remains to be fully elucidated, although as of 2009 great progress is currently being made in this respect with the generation of receptor subtype-specific knockout mice,^[3][4] and the first selective ligands for galanin receptor subtypes. Selective galanin agonists are anticonvulsant,^[5][6][7] while antagonists produce antidepressant and anxiolytic effects in animals,^{[8][9][10][11][12]} so either agonist or antagonist ligands for the galanin receptors may be potentially therapeutic compounds in humans.

Ligands

Agonists

Non-selective

• Galanin
• Galanin 1-15 fragment
• Galanin-like peptide - agonist at GAL₁ and GAL₂ but not GAL₃
• Galmic^[13]
• Galnon^[14]
• NAX 5055^[15][16]
• D-Gal(7-Ahp)-B2^[17]

GAL₁ selective

• M617^[18]

GAL_1/2 selective

• M1154 - has no GalR3 interaction^[19]

GAL₂ selective

• Galanin 2-11 amide - also called AR-M 1896, anticonvulsant in mice, CAS# 367518-31-8
• M1145 - selective compared to both GalR1 and GalR3 ^[20]
• M1153 - selective compared to both GalR1 and GalR3^[21]
• CYM 2503 (positive allosteric modulator)^[22]

Antagonists

Non-selective

• M35 peptide

GAL₁ selective

• SCH-202,596

GAL₂ selective

• M871 peptide^[18]

GAL₃ selective

• SNAP-37889^[23]
• SNAP-398,299^[24][25]