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Galanin receptor
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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.
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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]
- 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 - 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
- GAL2 selective
- M871 peptide[18]
- GAL3 selective
- SNAP-37889[23]
- SNAP-398,299[24][25]
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References
External links
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