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.
^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. PMID17604107.
^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. PMID10689365.
^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. PMID16854525. S2CID39707220.
^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. PMID17511615.
^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. PMID18500640. S2CID27882520.
^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. PMID18172432. S2CID10273560.
^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. PMID17637475. S2CID25988178.
^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. PMID19053761.
^ abSollenberg 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. S2CID36850989.
^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. PMID19467704. S2CID36222036.
^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. PMID21333705. S2CID23682808.
^Mittapalli, GK; et al. (2014). "Structure Activity Relationships of Novel Antiepileptic Drugs". Curr Med Chem. 21 (6): 722–54. doi:10.2174/0929867320666131119153215. PMID24251563.
^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. PMID16863269. S2CID13601784.
^Khan, SA, Zia, K, Ashraf, S, khan, A, Ul-Haq, Z (October 2021). "Theoretical investigation of selective ligand binding mode of galanin receptors". Journal of Biomolecular Structure and Dynamics. doi:10.1080/07391102.2021.1977703. PMID34632940.
External links[]
"Galanin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Galanin+Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
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Cell surface receptor: G protein-coupled receptors