Galaninski receptor

Galaninski receptor 1 Identifikatori Simbol GALR1 Alt. simboli GALNR1, GALNR Entrez 2587 HUGO 4132 OMIM 600377 RefSeq NM_001480 UniProt P47211 Drugi podaci Lokus Hromozom 18 q23

Galaninski receptor 2 Identifikatori Simbol GALR2 Entrez 8811 HUGO 4133 OMIM 603691 RefSeq NM_003857 UniProt O43603 Drugi podaci Lokus Hromozom 17 q25.3

Galaninski receptor 3 Identifikatori Simbol GALR3 Entrez 8484 HUGO 4134 OMIM 603692 RefSeq NM_003614 UniProt O60755 Drugi podaci Lokus Hromozom 22 q12.2-13.1

Galaninski receptor je G protein-spregnuti receptor, ili metabotropni receptor koji vezuje galanin.^[1]

Galaninski receptori se mogu naći u perifernom i centralnom nervnom sistemu kao i u endokrinom sistemu. Do sada je poznato da postoje tri tipa: GAL-R1, GAL-R2, i GAL-R3.^[2] Specifična funkcija svih podtipova nije potpuno istražena. Nedavno je došlo do napretka u pravljenju podtip-specifičnih nokaut miševa,^[3][4] i prvih selektivnih liganda galaninskih receptorskih podtipova. Selektivni galaninski agonisti su antiepileptici,^[5][6][7] dok su antagonisti antidepresanti i anksiolitici u životinjskim studijama,^{[8][9][10][11][12]}, tako da bilo agonisti ili antagonisti galaninskog receptora mogu potencijalno biti lekovi.

Ligandi

Agonisti

Neselektivni

• Galanin
• Galanin 1-15 fragment
• Galaninu sličan peptid - agonist GAL₁ i GAL₂, ali ne GAL₃ receptora
• Galmik^[13]
• Galnon^[14]
• NAX 5055^[15][16]

GAL₁ selektivni

• M617 peptid

GAL₂ selektivni

• Galanin 2-11 amid - takođe poznat kao AR-M 1896, antikonvulziv kod miševa, CAS# 367518-31-8
• M1145 - selektivan u odnosu na GalR1 i GalR3^[17]

Antagonisti

Neselektivni

• M35 peptid

GAL₁ selektivni

• SCH-202,596

GAL₂ selektivni

• M871 peptid

GAL₃ selektivni

• SNAP-37889 ^[18]
• SNAP-398,299^[19]

Literatura

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”. 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. 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 : CMLS 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. 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 : CMLS 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 : Official Publication of the American College of 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. 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 : the Journal of the American Society for Experimental NeuroTherapeutics 6 (2): 372–80. DOI:10.1016/j.nurt.2009.01.001. PMID 19332332. 
17. 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. 
18. 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. PMID 16863269. 
19. 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. DOI:10.1073/pnas.0508970102. PMC 1283534. PMID 16287967. 

Vanjske veze

• „Galaninski receptori”. IUPHAR baza podataka receptora i jonskih kanala. Internacionalna unija za baznu i kliničku farmakologiju. Arhivirano iz originala na datum 2016-03-03. 
• MeSH Galanin+Receptors