Galanin receptor

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galanin receptor 1
Alt. symbolsGALNR1, GALNR
Other data
LocusChr. 18 q23
galanin receptor 2
Other data
LocusChr. 17 q25.3
galanin receptor 3
Other data
LocusChr. 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.



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]


  • M35 peptide
GAL1 selective
GAL2 selective
GAL3 selective


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  2. Branchek TA, Smith KE, Gerald C, Walker MW (2000). "Galanin receptor subtypes". Trends Pharmacol. Sci. 21 (3): 109–17. doi:10.1016/S0165-6147(00)01446-2. PMID 10689365.
  3. 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.
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  8. Lu X, Barr AM, Kinney JW, Sanna P, Conti B, Behrens MM, Bartfai T (January 2005). "A role for galanin in antidepressant actions with a focus on the dorsal raphe nucleus". Proceedings of the National Academy of Sciences of the United States of America. 102 (3): 874–9. Bibcode:2005PNAS..102..874L. doi:10.1073/pnas.0408891102. PMC 545581. PMID 15647369.
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  10. 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.
  11. Kuteeva E, Hökfelt T, Wardi T, Ogren SO (June 2008). "Galanin, galanin receptor subtypes and depression-like behaviour". Cellular and Molecular Life Sciences. 65 (12): 1854–63. doi:10.1007/s00018-008-8160-9. PMID 18500640.
  12. 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.
  13. Ceide SC, Trembleau L, Haberhauer G, Somogyi L, Lu X, Bartfai T, Rebek J (November 2004). "Synthesis of galmic: a nonpeptide galanin receptor agonist". Proceedings of the National Academy of Sciences of the United States of America. 101 (48): 16727–32. Bibcode:2004PNAS..10116727C. doi:10.1073/pnas.0407543101. PMC 534730. PMID 15557002.
  14. 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.
  15. 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.
  16. White HS, Scholl EA, Klein BD, Flynn SP, Pruess TH, Green BR, Zhang L, Bulaj G (April 2009). "Developing novel antiepileptic drugs: characterization of NAX 5055, a systemically-active galanin analog, in epilepsy models". Neurotherapeutics. 6 (2): 372–80. doi:10.1016/j.nurt.2009.01.001. PMC 4402707. PMID 19332332.
  17. Robertson, CR; et al. (May 2012). "Generating orally active galanin analogues with analgesic activities". ChemMedChem. 7 (5): 903–9. doi:10.1002/cmdc.201100574. PMC 4332549. PMID 22374865.
  18. 18.0 18.1 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.
  19. Runesson J, Saar I, Sillard R, Langel U (2010). "M1154 – A Novel Galanin Ligand to Delineate the Galaninergic System". Proceedings of the 31st European Peptide Symposium: 452–453.
  20. Runesson J, Saar I, Lundström L, Järv J, Langel U (2009). "A novel GalR2-specific peptide agonist". Neuropeptides. 43 (3): 187–92. doi:10.1016/j.npep.2009.04.004. PMID 19467704.
  21. Saar I, Runesson J, McNamara I, Järv J, Robinson JK, Langel U (2011). "Novel galanin receptor subtype specific ligands in feeding regulation". Neurochemistry International. 58 (6): 714–720. doi:10.1016/j.neuint.2011.02.012. PMID 21333705.
  22. Mittapalli, GK; et al. (2014). "Structure Activity Relationships of Novel Antiepileptic Drugs". Curr Med Chem. 21 (6): 722–54. doi:10.2174/0929867320666131119153215. PMID 24251563.
  23. Ogren SO, Kuteeva E, Hökfelt T, Kehr J (2006). "Galanin receptor antagonists : a potential novel pharmacological treatment for mood disorders". CNS Drugs. 20 (8): 633–54. doi:10.2165/00023210-200620080-00003. PMID 16863269.
  24. 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.

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