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γ-氨基丁酸β受體

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γ-氨基丁酸（GABA）β受體1
識別
符號 GABBR1
Entrez 2550
HUGO 4070
OMIM 603540
RefSeq NM_021905
UniProt Q9UBS5
其他資料
基因座 6 p21.3
γ-氨基丁酸（GABA）β受體2
識別
符號 GABBR2
替換符號 GPR51
Entrez 9568
HUGO 4507
OMIM 607340
RefSeq NM_005458
UniProt O75899
其他資料
基因座 9 q22.1-22.3

γ-氨基丁酸β受體（又名GABABR）是代謝型γ-氨基丁酸（GABA）跨膜受體，其通過G蛋白與鉀通道連接。[1]在動作電位結束時，鉀濃度的變化使細胞超極化。GABAB介導的IPSP的翻轉電位為-100mV，其比GABAA IPSP更加超極化。GABAB受體存在於中樞神經系統和周圍神經系統的自主神經分叉中。[2]

該受體首先在1981年被確定，由Norman Bowery和他的團隊使用放射性標記的巴氯芬確定其在中樞神經系統中的分布。[3]

功能

該受體的激活可以刺激K+通道的開放，使神經元更接近K+的平衡電位。這降低了動作電位的頻率，從而減少了神經遞質的釋放。因此，GABAB受體是抑制性受體。[來源請求]

研究顯示通過使用具有Gi /G0α亞基的G蛋白，GABAB受體的激活還降低腺苷酸環化酶和Ca2+通道的活性。[4]

GABAB受體參與乙醇[5]，γ-羥基丁酸（GHB）[6]，並可能在疼痛[7]的生理作用。最近的研究表明，這些受體可能發揮更重要的作用。[8]

配體

激動劑

正向異構調節劑

拮抗劑

參考文獻

  1. ^ Chen, Kun; Li, Hong-Zhao; Ye, Na; Zhang, Jun; Wang, Jian-Jun. Role of GABAB receptors in GABA and baclofen-induced inhibition of adult rat cerebellar interpositus nucleus neurons in vitro. Brain Research Bulletin. 2005-10-30, 67 (4): 310–318 [2018-08-17]. ISSN 0361-9230. PMID 16182939. doi:10.1016/j.brainresbull.2005.07.004. （原始內容存檔於2019-05-09）. 
  2. ^ Hyland, Niall P.; Cryan, John F. A Gut Feeling about GABA: Focus on GABAB Receptors. Frontiers in Pharmacology. 2010-10-04, 1 [2018-08-17]. ISSN 1663-9812. PMC 3153004 可免費查閱. PMID 21833169. doi:10.3389/fphar.2010.00124. （原始內容存檔於2020-11-12）. 
  3. ^ Hill, D. R.; Bowery, N. G. 3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABA B sites in rat brain. Nature. 1981-03-12, 290 (5802): 149–152 [2018-08-17]. ISSN 0028-0836. PMID 6259535. （原始內容存檔於2019-05-09）. 
  4. ^ P,, Rang, H.; 1945-, Flower, R. J. (Rod J.),; (Graeme),, Henderson, G. Rang and Dale's pharmacology Eighth edition. [United Kingdom]. ISBN 9780702053627. OCLC 903083639. 
  5. ^ Dzitoyeva, Svetlana; Dimitrijevic, Nikola; Manev, Hari. γ-Aminobutyric acid B receptor 1 mediates behavior-impairing actions of alcohol in Drosophila: Adult RNA interference and pharmacological evidence. Proceedings of the National Academy of Sciences of the United States of America. 2003-04-29, 100 (9): 5485–5490 [2018-08-17]. ISSN 0027-8424. PMC 154371 可免費查閱. PMID 12692303. doi:10.1073/pnas.0830111100. （原始內容存檔於2022-02-05）. 
  6. ^ Dimitrijevic, Nikola; Dzitoyeva, Svetlana; Satta, Rosalba; Imbesi, Marta; Yildiz, Sevim; Manev, Hari. Drosophila GABAB receptors are involved in behavioral effects of γ-hydroxybutyric acid (GHB). European Journal of Pharmacology. 2005-09, 519 (3): 246–252 [2018-08-17]. ISSN 0014-2999. doi:10.1016/j.ejphar.2005.07.016. （原始內容存檔於2020-10-01）. 
  7. ^ Manev, Hari; Dimitrijevic, Nikola. Drosophila model for in vivo pharmacological analgesia research. European Journal of Pharmacology. 2004-05, 491 (2-3): 207–208 [2018-08-17]. ISSN 0014-2999. doi:10.1016/j.ejphar.2004.03.030. （原始內容存檔於2020-02-29）. 
  8. ^ Dzitoyeva, Svetlana; Gutnov, Alan; Imbesi, Marta; Dimitrijevic, Nikola; Manev, Hari. Developmental role of GABAB(1) receptors in Drosophila. Brain Research. Developmental Brain Research. 2005-08-08, 158 (1-2): 111–114 [2018-08-17]. ISSN 0165-3806. PMID 16054235. doi:10.1016/j.devbrainres.2005.06.005. （原始內容存檔於2019-05-09）. 
  9. ^ Paterson, Neil E.; Vlachou, Styliani; Guery, Sebastien; Kaupmann, Klemens; Froestl, Wolfgang; Markou, Athina. Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. The Journal of Pharmacology and Experimental Therapeutics. 2008-7, 326 (1): 306–314 [2018-08-17]. ISSN 1521-0103. PMC 2574924 可免費查閱. PMID 18445779. doi:10.1124/jpet.108.139204. （原始內容存檔於2019-05-09）. 
  10. ^ Urwyler, Stephan; Pozza, Mario F.; Lingenhoehl, Kurt; Mosbacher, Johannes; Lampert, Christina; Froestl, Wolfgang; Koller, Manuel; Kaupmann, Klemens. N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. The Journal of Pharmacology and Experimental Therapeutics. 2003-10, 307 (1): 322–330 [2018-08-18]. ISSN 0022-3565. PMID 12954816. doi:10.1124/jpet.103.053074. （原始內容存檔於2019-05-10）. 
  11. ^ Urwyler, S.; Mosbacher, J.; Lingenhoehl, K.; Heid, J.; Hofstetter, K.; Froestl, W.; Bettler, B.; Kaupmann, K. Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Molecular Pharmacology. 2001-11, 60 (5): 963–971 [2018-08-18]. ISSN 0026-895X. PMID 11641424. （原始內容存檔於2019-05-10）. 
  12. ^ Adams, C. L.; Lawrence, A. J. CGP7930: a positive allosteric modulator of the GABAB receptor. CNS drug reviews. 2007, 13 (3): 308–316 [2018-08-18]. ISSN 1080-563X. PMID 17894647. doi:10.1111/j.1527-3458.2007.00021.x. （原始內容存檔於2019-05-09）. 
  13. ^ Giotti, A.; Luzzi, S.; Spagnesi, S.; Zilletti, L. Homotaurine: a GABAB antagonist in guinea-pig ileum. British Journal of Pharmacology. 1983-8, 79 (4): 855–862 [2018-08-17]. ISSN 0007-1188. PMC 2044932 可免費查閱. PMID 6652358. （原始內容存檔於2019-05-10）. 
  14. ^ Kimura, T.; Saunders, P.A.; Kim, H.S.; Rheu, H.M.; Oh, K.W.; Ho, I.K. Interactions of ginsenosides with ligand-bindings of GABAA and GABAB receptors. General Pharmacology: The Vascular System. 1994-01, 25 (1): 193–199 [2018-08-17]. ISSN 0306-3623. doi:10.1016/0306-3623(94)90032-9. （原始內容存檔於2019-05-10）. 
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