The galanin receptor is a G protein-coupled receptor, or metabotropic receptor which binds galanin.[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.
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 - 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
- GAL1 selective
- GAL2 selective
- GAL3 selective
Lang R, Gundlach AL, Kofler B (2007). "The galanin peptide family: receptor pharmacology, pleiotropic biological actions, and implications in health and disease". Pharmacol. Ther. 115 (2): 177–207. doi:10.1016/j.pharmthera.2007.05.009. PMID 17604107.
Rustay NR, Wrenn CC, Kinney JW, Holmes A, Bailey KR, Sullivan TL, Harris AP, Long KC, Saavedra MC, Starosta G, Innerfield CE, Yang RJ, Dreiling JL, Crawley JN (June 2005). "Galanin impairs performance on learning and memory tasks: findings from galanin transgenic and GAL-R1 knockout mice". Neuropeptides. 39 (3): 239–43. doi:10.1016/j.npep.2004.12.026. PMID 15944016. S2CID 32791271.
Barr AM, Kinney JW, Hill MN, Lu X, Biros S, Rebek J, Bartfai T (September 2006). "A novel, systemically active, selective galanin receptor type-3 ligand exhibits antidepressant-like activity in preclinical tests". Neuroscience Letters. 405 (1–2): 111–5. doi:10.1016/j.neulet.2006.06.033. PMID 16854525. S2CID 39707220.
Lu X, Sharkey L, Bartfai T (June 2007). "The brain galanin receptors: targets for novel antidepressant drugs". CNS & Neurological Disorders Drug Targets. 6 (3): 183–92. doi:10.2174/187152707780619335. PMID 17511615.
Kuteeva E, Wardi T, Lundström L, Sollenberg U, Langel U, Hökfelt T, Ogren SO (October 2008). "Differential role of galanin receptors in the regulation of depression-like behavior and monoamine/stress-related genes at the cell body level". Neuropsychopharmacology. 33 (11): 2573–85. doi:10.1038/sj.npp.1301660. PMID 18172432. S2CID 10273560.
Rajarao SJ, Platt B, Sukoff SJ, Lin Q, Bender CN, Nieuwenhuijsen BW, Ring RH, Schechter LE, Rosenzweig-Lipson S, Beyer CE (October 2007). "Anxiolytic-like activity of the non-selective galanin receptor agonist, galnon". Neuropeptides. 41 (5): 307–20. doi:10.1016/j.npep.2007.05.001. PMID 17637475. S2CID 25988178.
Bulaj G, Green BR, Lee HK, Robertson CR, White K, Zhang L, Sochanska M, Flynn SP, Scholl EA, Pruess TH, Smith MD, White HS (December 2008). "Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities". Journal of Medicinal Chemistry. 51 (24): 8038–47. doi:10.1021/jm801088x. PMID 19053761.
Sollenberg UE, Runesson J, Sillard R, Langel U (March 2010). "Binding of Chimeric Peptides M617 and M871 to Galanin Receptor Type 3 Reveals Characteristics of Galanin Receptor–Ligand Interaction". International Journal of Peptide Research and Therapeutics. 16 (1): 17–22. doi:10.1007/s10989-009-9197-9. S2CID 36850989.
Swanson CJ, Blackburn TP, Zhang X, Zheng K, Xu ZQ, Hökfelt T, Wolinsky TD, Konkel MJ, Chen H, Zhong H, Walker MW, Craig DA, Gerald CP, Branchek TA (November 2005). "Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299". Proceedings of the National Academy of Sciences of the United States of America. 102 (48): 17489–94. Bibcode:2005PNAS..10217489S. doi:10.1073/pnas.0508970102. PMC 1283534. PMID 16287967.