Galanin receptor

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galanin receptor 1
Identifiers
Symbol GALR1
Alt. symbols GALNR1, GALNR
Entrez 2587
HUGO 4132
OMIM 600377
RefSeq NM_001480
UniProt P47211
Other data
Locus Chr. 18 q23
galanin receptor 2
Identifiers
Symbol GALR2
Entrez 8811
HUGO 4133
OMIM 603691
RefSeq NM_003857
UniProt O43603
Other data
Locus Chr. 17 q25.3
galanin receptor 3
Identifiers
Symbol GALR3
Entrez 8484
HUGO 4134
OMIM 603692
RefSeq NM_003614
UniProt O60755
Other data
Locus Chr. 22 q12.2-13.1

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

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
GAL1 selective


GAL1/2 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 - seletive compared to both GalR1 and GalR3 [20]
  • M1153 - seletive compared to both GalR1 and GalR3[21]
  • CYM 2503 (positive allosteric modulator)[22]

Antagonists

Non-selective
  • M35 peptide
GAL1 selective
GAL2 selective
GAL3 selective

References

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External links

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