γ-氨基丁酸β受体

γ-氨基丁酸（GABA）β受体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（GABA）β受体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β受体（又名GABA_BR）是代谢型γ-氨基丁酸（GABA）跨膜受体，其通过G蛋白与钾通道连接。^[1]在动作电位结束时，钾浓度的变化使细胞超极化。GABA_B介导的IPSP的翻转电位为-100mV，其比GABA_A IPSP更加超极化。GABA_B受体存在于中枢神经系统和周围神经系统的自主神经分叉中。^[2]

该受体首先在1981年被确定，由Norman Bowery和他的团队使用放射性标记的巴氯芬确定其在中枢神经系统中的分布。^[3]

功能

该受体的激活可以刺激K⁺通道的开放，使神经元更接近K⁺的平衡电位。这降低了动作电位的频率，从而减少了神经递质的释放。因此，GABA_B受体是抑制性受体。^{[來源請求]}

研究显示通过使用具有Gi /G0α亚基的G蛋白，GABA_B受体的激活还降低腺苷酸环化酶和Ca2⁺通道的活性。^[4]

GABA_B受体参与乙醇^[5]，γ-羟基丁酸（GHB）^[6]，并可能在疼痛^[7]的生理作用。最近的研究表明，这些受体可能发挥更重要的作用。^[8]

配体

激动剂

GABA
巴氯芬
γ-羟基丁酸
异缬氨酸
菲尼布特（β-苯基-γ-丁酸）
3-氨基丙基次膦酸（英语：3-Aminopropylphosphinic acid）
Lesogaberan

正向异构调节剂

芬地林（英语：Fendiline）
BHF-177^[9]
BHFF
BSPP
GS-39783（英语：GS-39783）^[10]
CGP-7930^[11]^[12]

拮抗剂

参考文献

^ 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. （原始内容存档于2019-05-09）.
^ 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 . PMID 21833169. doi:10.3389/fphar.2010.00124. （原始内容存档于2020-11-12）.
^ 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. （原始内容存档于2019-05-09）.
^ 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.
^ 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 . PMID 12692303. doi:10.1073/pnas.0830111100. （原始内容存档于2022-02-05）.
^ 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. （原始内容存档于2020-10-01）.
^ 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. （原始内容存档于2020-02-29）.
^ 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. （原始内容存档于2019-05-09）.
^ 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 . PMID 18445779. doi:10.1124/jpet.108.139204. （原始内容存档于2019-05-09）. 请检查|date=中的日期值 (帮助)
^ 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. （原始内容存档于2019-05-10）.
^ 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. （原始内容存档于2019-05-10）.
^ 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. （原始内容存档于2019-05-09）.
^ 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 . PMID 6652358. （原始内容存档于2019-05-10）. 请检查|date=中的日期值 (帮助)
^ 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. （原始内容存档于2019-05-10）.

[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. （原始内容存档于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 . PMID 21833169. doi:10.3389/fphar.2010.00124. （原始内容存档于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. （原始内容存档于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 . PMID 12692303. doi:10.1073/pnas.0830111100. （原始内容存档于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. （原始内容存档于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. （原始内容存档于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. （原始内容存档于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 . PMID 18445779. doi:10.1124/jpet.108.139204. （原始内容存档于2019-05-09）. 请检查|date=中的日期值 (帮助)

[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. （原始内容存档于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. （原始内容存档于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. （原始内容存档于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 . PMID 6652358. （原始内容存档于2019-05-10）. 请检查|date=中的日期值 (帮助)

[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. （原始内容存档于2019-05-10）.

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