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

2

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. 

Spoljašnje 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
  • p
  • r
  • u
Klasa A: Rodopsinu slični
α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
Adenozinski (A1, A2A, A2B, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(svi osim 5-HT3) 5-HT1 (A, B, D, E, F) • 5-HT2 (A, B, C) • 5-HT (4, 5A, 6, 7)
Drugi
Acetilholin (M1, M2, M3, M4, M5) • Dopamin (D1, D2, D3, D4, D5) • Histamin (H1, H2, H3, H4) • Melatonin (1A, 1B, 1C) • TAAR (1, 2, 3, 5, 6, 8, 9)
Metaboliti i
signalni molekuli
CysLT (1, 2) • LTB4 (1, 2) • FPRL1 • OXE • Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) • Prostaciklin • Tromboksan
Drugi
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat  • Lizofosfatidna kiselina (1, 2, 3, 4, 5, 6)  • Lizofosfolipid (1, 2, 3, 4, 5, 6, 7, 8) • Niacin (1, 2) • Oksoglutarat • PAF • Sfingozin-1-fosfat (1, 2, 3, 4, 5) • Sukcinat
Peptid
B/W (1, 2) • FF (1, 2) • S • Y (1, 2, 4, 5) • Neuromedin (B, U (1, 2)) • Neurotenzin (1, 2)
Drugi
Anafilatoksin (C3a, C5a) • Angiotenzin (1, 2) • Apelin • Bombezin (BRS3, GRPR, NMBR) • Bradikinin (B1, B2) • Hemokin • Holecistokinin (A, B) • Endotelin (A, B) • Formil peptid (1, 2, 3) • FSH • Galanin (1, 2, 3) • GHB receptor • Gonadotropin-oslobađajući hormon (1, 2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) • Melanokortin (1, 2, 3, 4, 5) • MCHR (1, 2) • Motilin • Opioidni (δ, κ, μ, Nociceptin & ζ, ali ne σ) • Oreksin (1, 2) • Oksitocin • Prokineticin (1, 2) • Prolaktin-oslobađajući peptid • Relaksin (1, 2, 3, 4) • Somatostatin (1, 2, 3, 4, 5) • Tahikinin (1, 2, 3) • Tirotropin • Tirotropin-oslobađajući hormon • Urotenzin-II • Vazopresin (1A, 1B, 2)
Razno
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Drugi
Adrenomedulin • Mirisni • Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) • Proteazom-aktivirani (1, 2, 3, 4) • SREB (1, 2, 3)
Klasa B: Sekretinu slični
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Drugi
Klasa C: Metabotropni
glutamat / feromon
TAS1R (1, 2, 3) • TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Drugi
Klasa F:
Frizzled / Zaglađeni
Uvojiti
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Zaglađeni
B trdu: peptidi (nrpl/grfl/cytl/horl), receptori (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd, signalni putevi (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
  • p
  • r
  • u
Neuropeptidni receptori
Hormonski receptori
Drugi
Opioidni receptori
Drugi neuropeptidni receptori
B trdu: peptidi (nrpl/grfl/cytl/horl), receptori (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd, signalni putevi (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
  • p
  • r
  • u
Holecistokinin
CCKA
Agonisti: Holecistokinin • CCK-4
Antagonisti: Asperlicin • Proglumid • Lorglumid • Devazepid • Deksloksiglumid
CCKB
Agonisti: Holecistokinin • CCK-4 • Gastrin
Antagonisti: Proglumid • CI-988
CRH
CRF1
CRF2
Galanin
GAL1
Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL2
Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL3
Agonisti: Galanin • Galmic • Galnon
Grelin
Agonisti: Grelin • Kapromorelin • MK-677 • Sermorelin • SM-130,686 • Tabimorelin
MCH
MCH1
MCH2
Melanokortin
MC1
MC2
Agonisti: ACTH • Kosintropin • Tetrakosaktid
MC3
Agonisti: alfa-MSH • Bremelanotid • Melanotan II
MC4
Agonisti: alfa-MSH • Bremelanotid • Melanotan II • THIQ
Antagonisti: Agutiju srodni peptid
MC5
Agonisti: alfa-MSH • Melanotan II
Neuropeptid S
Agonisti: Neuropeptid S
Antagonisti: SHA-68
Neuropeptid Y
Y1
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: BIBP-3226
Y2
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: BIIE-0246
Y4
Agonisti: Neuropeptid Y • Pankreasni polipeptid • Peptid YY
Antagonisti: UR-AK49
Y5
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: Lu AA-33810
Neurotenzin
NTS1
Agonisti: Neurotenzin • Neuromedin N
Antagonisti: SR-48692 • SR-142,948
NTS2
Agonisti: Neurotenzin
Antagonisti: Levokabastin • SR-142,948
Opioid
vidi Opioidi
Oreksin
OX1
Agonisti: Oreksin-A
Antagonisti: Almoreksant • SB-334,867 • SB-408,124 • SB-649,868
OX2
Agonisti: Oreksin-A
Antagonisti: Almoreksant • SB-649,868 • TCS-OX2-29
Oksitocin
Agonisti: Karbetocin • Demoksitocin • Oksitocin • WAY-267,464
Antagonisti: Atosiban • L-371,257 • L-368,899
Tahikinin
NK1
Agonisti: Supstanca P
Antagonisti: Aprepitant • Befetupitant • Kasopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • Vofopitant
NK2
Agonisti: Neurokinin A
Antagonisti: GR-159897 • Ibodutant • Saredutant
NK3
Agonisti: Neurokinin B
Antagonisti: Osanetant • Talnetant
Vazopresin
V1A
Agonisti: Dezmopresin • Felipresin • Ornipresin • Terlipresin • Vazopresin
Antagonisti: Konivaptan • Demeklociklin • Relkovaptan
V1B
Agonisti: Felipresin • Ornipresin • Terlipresin • Vazopresin
Antagonisti: Demeklociklin • Nelivaptan
V2
Agonisti: Dezmopresin • Ornipresin • Vazopresin
Antagonisti: Konivaptan • Demeklociklin • Liksivaptan • Mozavaptan • Satavaptan • Tolvaptan