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
- GAL1 selective
- GAL2 selective
- GAL3 selective
References
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External links
