依托咪酯、丙泊酚和戊巴比妥对人5-羟色胺（3A）和5-羟色胺（3AB）受体的抑制作用。
Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital.
作者信息
Rüsch Dirk, Braun Hans A, Wulf Hinnerk, Schuster Anika, Raines Douglas E
机构信息
Department of Anaesthesia and Critical Care, University Hospital Giessen-Marburg GmbH, Marburg Campus, Baldingerstrasse, 35033 Marburg, Germany.
出版信息
Eur J Pharmacol. 2007 Nov 14;573(1-3):60-4. doi: 10.1016/j.ejphar.2007.07.009. Epub 2007 Jul 13.
Abstract
The actions of intravenous anaesthetics on 5-HT(3AB) receptors have not been studied. Using oocyte electrophysiology, the effects of etomidate, propofol, and pentobarbital on human 5-HT(3A) and 5-HT(3AB) receptors were studied and compared. Inhibition of peak currents by all three compounds in both receptor subtypes was anaesthetic concentration-dependant and non-competitive. Because the half-maximal inhibitory concentrations for etomidate, propofol and pentobarbital in 5-HT(3A) and 5-HT(3AB) receptors were all above their respective anaesthetic concentrations, the results of our study suggest that neither 5-HT(3) receptor subtype contributes to the anaesthetic actions of etomidate, propofol or pentobarbital.
摘要
静脉麻醉药对5-HT(3AB)受体的作用尚未得到研究。运用卵母细胞电生理学方法，研究并比较了依托咪酯、丙泊酚和戊巴比妥对人5-HT(3A)和5-HT(3AB)受体的影响。这三种化合物对两种受体亚型的峰值电流的抑制作用均呈麻醉浓度依赖性且为非竞争性。由于依托咪酯、丙泊酚和戊巴比妥在5-HT(3A)和5-HT(3AB)受体中的半数最大抑制浓度均高于其各自的麻醉浓度，我们的研究结果表明，5-HT(3)受体亚型均不参与依托咪酯、丙泊酚或戊巴比妥的麻醉作用。
相似文献
1
Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital.依托咪酯、丙泊酚和戊巴比妥对人5-羟色胺（3A）和5-羟色胺（3AB）受体的抑制作用。
Eur J Pharmacol. 2007 Nov 14;573(1-3):60-4. doi: 10.1016/j.ejphar.2007.07.009. Epub 2007 Jul 13.
2
The interaction of general anaesthetics with recombinant GABAA and glycine receptors expressed in Xenopus laevis oocytes: a comparative study.全身麻醉药与非洲爪蟾卵母细胞中表达的重组γ-氨基丁酸A型（GABAA）和甘氨酸受体的相互作用：一项比较研究。
Br J Pharmacol. 1997 Dec;122(8):1707-19. doi: 10.1038/sj.bjp.0701563.
3
Subunit-dependent modulation of the 5-hydroxytryptamine type 3 receptor open-close equilibrium by n-alcohols.正构醇对5-羟色胺3型受体开闭平衡的亚基依赖性调节
J Pharmacol Exp Ther. 2007 Jun;321(3):1069-74. doi: 10.1124/jpet.106.118752. Epub 2007 Mar 7.
4
Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate is a novel positive modulator of GABAA receptors.2-(4-溴苯基)-1-(2,4-二氯苯基)-1H-咪唑-4-羧酸乙酯是一种新型的GABAA受体正向调节剂。
Eur J Pharmacol. 2005 Jun 15;516(3):204-11. doi: 10.1016/j.ejphar.2005.05.006.
5
The effects of a point mutation of the beta2 subunit of GABA(A) receptor on direct and modulatory actions of general anesthetics.γ-氨基丁酸A（GABA(A)）受体β2亚基点突变对全身麻醉药直接作用和调节作用的影响
Eur J Pharmacol. 1999 Mar 5;368(2-3):269-76. doi: 10.1016/s0014-2999(99)00033-3.
6
The pyrrole etomidate analog carboetomidate potently inhibits human 5-HT3A receptor function: comparisons with etomidate and potential implications for emetogenesis.吡咯依托咪酯类似物卡泊依托咪酯能强效抑制人 5-HT3A 受体功能：与依托咪酯的比较及对催吐作用的潜在影响。
Anesth Analg. 2013 Mar;116(3):573-9. doi: 10.1213/ANE.0b013e31827d204d. Epub 2013 Feb 11.
7
General anesthetic-induced channel gating enhancement of 5-hydroxytryptamine type 3 receptors depends on receptor subunit composition.全身麻醉诱导的5-羟色胺3型受体通道门控增强取决于受体亚基组成。
J Pharmacol Exp Ther. 2005 Nov;315(2):771-6. doi: 10.1124/jpet.105.090621. Epub 2005 Aug 4.
8
Subunit-dependent interaction of the general anaesthetic etomidate with the gamma-aminobutyric acid type A receptor.全身麻醉药依托咪酯与γ-氨基丁酸A型受体的亚基依赖性相互作用。
Br J Pharmacol. 1997 Mar;120(5):749-56. doi: 10.1038/sj.bjp.0700927.
9
Recombinant human 5-HT3A receptors in outside-out patches of HEK 293 cells: basic properties and barbiturate effects.重组人5-HT3A受体在HEK 293细胞外向膜片钳中的基本特性及巴比妥酸盐的作用。
Naunyn Schmiedebergs Arch Pharmacol. 2000 Sep;362(3):255-65. doi: 10.1007/s002100000288.
10
Functional sites involved in modulation of the GABAA receptor channel by the intravenous anesthetics propofol, etomidate and pentobarbital.静脉麻醉药丙泊酚、依托咪酯和戊巴比妥对GABAA受体通道进行调节所涉及的功能位点。
Neuropharmacology. 2016 Jun;105:207-214. doi: 10.1016/j.neuropharm.2016.01.003. Epub 2016 Jan 6.
引用本文的文献
1
International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.国际基础和临床药理学联合会。CX. 5-羟色胺受体分类：药理学与功能。
Pharmacol Rev. 2021 Jan;73(1):310-520. doi: 10.1124/pr.118.015552.
2
Management of severe arterial hypertension associated with serotonin syndrome: a case report analysis based on systematic review techniques.与血清素综合征相关的重度动脉高血压的管理：基于系统评价技术的病例报告分析
Ther Adv Psychopharmacol. 2019 Mar 11;9:2045125318818814. doi: 10.1177/2045125318818814. eCollection 2019.
3
The Role of 5-HT3 Receptors in Signaling from Taste Buds to Nerves.5-羟色胺3型受体在从味蕾到神经的信号传导中的作用。
J Neurosci. 2015 Dec 2;35(48):15984-95. doi: 10.1523/JNEUROSCI.1868-15.2015.
4
Opposing effects of the anesthetic propofol at pentameric ligand-gated ion channels mediated by a common site.配体门控离子通道中共同作用位点介导的麻醉药异丙酚的拮抗作用。
J Neurosci. 2014 Feb 5;34(6):2155-9. doi: 10.1523/JNEUROSCI.4307-13.2014.
5
Discriminating between 5-HT₃A and 5-HT₃AB receptors.区分 5-HT₃A 和 5-HT₃AB 受体。
Br J Pharmacol. 2013 Jun;169(4):736-47. doi: 10.1111/bph.12166.
6
The pyrrole etomidate analog carboetomidate potently inhibits human 5-HT3A receptor function: comparisons with etomidate and potential implications for emetogenesis.吡咯依托咪酯类似物卡泊依托咪酯能强效抑制人 5-HT3A 受体功能：与依托咪酯的比较及对催吐作用的潜在影响。
Anesth Analg. 2013 Mar;116(3):573-9. doi: 10.1213/ANE.0b013e31827d204d. Epub 2013 Feb 11.
7
Therapeutics of 5-HT3 receptor antagonists: current uses and future directions.5-HT3 受体拮抗剂的治疗学：当前用途和未来方向。
Pharmacol Ther. 2011 Jun;130(3):338-47. doi: 10.1016/j.pharmthera.2011.02.003. Epub 2011 Feb 26.
8
Allosteric modulation of the 5-HT(3) receptor.5-羟色胺（5-HT）受体的变构调节。
Curr Opin Pharmacol. 2011 Feb;11(1):75-80. doi: 10.1016/j.coph.2011.01.010. Epub 2011 Feb 20.
9
Anesthetic sensitivity of the Gloeobacter violaceus proton-gated ion channel.紫色硫细菌质子门控离子通道的麻醉敏感性。
Anesth Analg. 2010 Jan 1;110(1):59-63. doi: 10.1213/ANE.0b013e3181c4bc69. Epub 2009 Nov 21.
本文引用的文献
1
Detection of human and rodent 5-HT3B receptor subunits by anti-peptide polyclonal antibodies.利用抗肽多克隆抗体检测人和啮齿动物的5-HT3B受体亚基。
BMC Neurosci. 2006 Mar 29;7:27. doi: 10.1186/1471-2202-7-27.
2
General anesthetic-induced channel gating enhancement of 5-hydroxytryptamine type 3 receptors depends on receptor subunit composition.全身麻醉诱导的5-羟色胺3型受体通道门控增强取决于受体亚基组成。
J Pharmacol Exp Ther. 2005 Nov;315(2):771-6. doi: 10.1124/jpet.105.090621. Epub 2005 Aug 4.
3
Modulation of human 5-hydroxytryptamine type 3AB receptors by volatile anesthetics and n-alcohols.挥发性麻醉剂和正醇类对人5-羟色胺3AB型受体的调节作用。
J Pharmacol Exp Ther. 2005 Jul;314(1):338-45. doi: 10.1124/jpet.105.085076. Epub 2005 Apr 14.
4
Activation of presynaptic 5-HT3 receptors facilitates glutamatergic synaptic inputs to area postrema neurons in rat brain slices.突触前5-羟色胺3型受体的激活促进了谷氨酸能突触输入到大鼠脑片中的最后区神经元。
Methods Find Exp Clin Pharmacol. 2004 Oct;26(8):615-22. doi: 10.1358/mf.2004.26.8.863726.
5
Cloning, physical mapping and expression analysis of the human 5-HT3 serotonin receptor-like genes HTR3C, HTR3D and HTR3E.人类5-羟色胺3型血清素受体样基因HTR3C、HTR3D和HTR3E的克隆、物理图谱绘制及表达分析。
Gene. 2003 May 22;310:101-11. doi: 10.1016/s0378-1119(03)00503-1.
6
Serotonin 5-HT(3) receptors in rat CA1 hippocampal interneurons: functional and molecular characterization.大鼠海马CA1区中间神经元中的5-羟色胺5-HT(3)受体：功能与分子特征
J Physiol. 2002 Nov 1;544(3):715-26. doi: 10.1113/jphysiol.2002.029736.
7
Differential composition of 5-hydroxytryptamine3 receptors synthesized in the rat CNS and peripheral nervous system.大鼠中枢神经系统和外周神经系统合成的5-羟色胺3受体的差异组成。
J Neurosci. 2002 Aug 1;22(15):6732-41. doi: 10.1523/JNEUROSCI.22-15-06732.2002.
8
Generation of a selective 5-HT3B subunit-recognising polyclonal antibody; identification of immunoreactive cells in rat hippocampus.
Neuropharmacology. 2001 Dec;41(8):1013-6. doi: 10.1016/s0028-3908(01)00153-8.
9
An electrophysiological study of the effects of propofol on native neuronal ligand-gated ion channels.丙泊酚对天然神经元配体门控离子通道作用的电生理研究。
Clin Exp Pharmacol Physiol. 2001 May-Jun;28(5-6):451-8. doi: 10.1046/j.1440-1681.2001.03469.x.
10
Recombinant human 5-HT3A receptors in outside-out patches of HEK 293 cells: basic properties and barbiturate effects.重组人5-HT3A受体在HEK 293细胞外向膜片钳中的基本特性及巴比妥酸盐的作用。
Naunyn Schmiedebergs Arch Pharmacol. 2000 Sep;362(3):255-65. doi: 10.1007/s002100000288.
Zotero 插件