Galanin receptor

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

galanin receptor 1
Identifiers
SymbolGALR1
Alt. symbolsGALNR1, GALNR
NCBI gene2587
HGNC4132
OMIM600377
RefSeqNM_001480
UniProtP47211
Other data
LocusChr. 18 q23
galanin receptor 2
Identifiers
SymbolGALR2
NCBI gene8811
HGNC4133
OMIM603691
RefSeqNM_003857
UniProtO43603
Other data
LocusChr. 17 q25.3
galanin receptor 3
Identifiers
SymbolGALR3
NCBI gene8484
HGNC4134
OMIM603692
RefSeqNM_003614
UniProtO60755
Other data
LocusChr. 22 q12.2-13.1

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 - 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
GAL3 selective
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References
  1. 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.
  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" (PDF). Neuropeptides. 39 (3): 239–43. doi:10.1016/j.npep.2004.12.026. PMID 15944016.
  4. Lu X, Ross B, Sanchez-Alavez M, Zorrilla EP, Bartfai T (August 2008). "Phenotypic analysis of GalR2 knockout mice in anxiety- and depression-related behavioral tests". Neuropeptides. 42 (4): 387–97. doi:10.1016/j.npep.2008.04.009. PMC 3399724. PMID 18554714.
  5. Mazarati A, Lundström L, Sollenberg U, Shin D, Langel U, Sankar R (August 2006). "Regulation of kindling epileptogenesis by hippocampal galanin type 1 and type 2 receptors: The effects of subtype-selective agonists and the role of G-protein-mediated signaling". The Journal of Pharmacology and Experimental Therapeutics. 318 (2): 700–8. doi:10.1124/jpet.106.104703. PMC 1508166. PMID 16699066.
  6. Lerner JT, Sankar R, Mazarati AM (June 2008). "Galanin and epilepsy". Cellular and Molecular Life Sciences. 65 (12): 1864–71. doi:10.1007/s00018-008-8161-8. PMID 18500639.
  7. Zhang L, Robertson CR, Green BR, Pruess TH, White HS, Bulaj G (February 2009). "Structural Requirements for a Lipoamino Acid in Modulating the Anticonvulsant Activities of Systemically Active Galanin Analogues". Journal of Medicinal Chemistry. 52 (5): 1310–6. doi:10.1021/jm801397w. PMC 2765488. PMID 19199479.
  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.
  9. 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.
  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. 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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