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全身麻醉药物分子靶点的研究进展 被引量:3

Advance of molecular targets for general anesthetics
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摘要 背景全身麻醉药物通过增强抑制性神经传递和减弱兴奋性神经传递在中枢神经系统中发挥作用。兴奋性神经递质如谷氨酸和乙酰胆碱(acetylcholine,ACh)引起去极化,而抑制性神经递质如γ-氨基丁酸(γ-aminobutyric acid,GABA)和甘氨酸通过超极化或分流兴奋性电流来降低突触后活性。目的探讨药物分子靶点在全身麻醉中的作用机制。内容就全身麻醉药物主要分子靶点作简要介绍。趋向针对麻醉药物分子靶点对全身麻醉的促进作用所进行的研究可能有助于研发出更有效且更安全的麻醉药。 Background General anesthetics produce widespread depression in the central nervous system by enhancing inhibitory neurotransmission and reducing excitatory neurotransmission. Excitatory neurotransmitters induce depolarization, such as glutamate and acetylcholine(ACh ). Whereas inhibitory neurotransmitters reduce postsynaptic activity by byperpolarization or shunting excitatory currents, such as γ-aminobutyric acid(GABA) and glycine. Objective To investigate the mechanisms of drug molecular targets in general anesthesia. Content In this review, we briefly introduce the research progress of drug molecular targets of general anesthesia. Trend Studies on the contributions of anesthetic targets to general anesthesia may facilitate the development of more effective and safer anesthetics.
出处 《国际麻醉学与复苏杂志》 CAS 2015年第5期463-466,共4页 International Journal of Anesthesiology and Resuscitation
基金 上海市浦东新区卫生系统优秀青年医学人才培养计划资助(PWRq20144-08)
关键词 分子靶点 受体 Γ-氨基丁酸 甘氨酸 乙酰胆碱 谷氨酸 钾通道 钠通道 Molecular targets Receptor γ-aminobutyric acid Glycine Acetylcholine Glutamate Potassium channels Sodium channels
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参考文献25

  • 1Belelli D, Harrison NL, Maguire J, et al. Extrasynaptic GABAareceptors: form, pharmacology, and function [J]. J Neurosci,2009, 29(41): 12757-12763.
  • 2高少龙,何绍明.全身麻醉药在蛋白模型和离子通道的分子靶位及变构调节机制[J].国际麻醉学与复苏杂志,2014,35(1):72-74. 被引量:3
  • 3Garcia PS, Kolesky SE, Jenkins A. General anesthetic actions onGABAa receptors[J]. Curr Neuropharmacol, 2010, 8( ] ): 2-9.
  • 4Farrant M, Nusser Z. Variations on an inhibitory theme : phasic andtonic activation of GABAa receptors[J], Nat Rev Neurosci, 2005, 6(3): 215-229.
  • 5Campagna JA, Miller KW,Forman SA. Mechanisms of actionsof inhaled anesthetics[J]. N Engl J Med, 2003, 348(21) : 2110-2124.
  • 6McCartney MR, Deeb TZ, Henderson TN, et al. Tonically activeGABAA receptors in hippocampal pyramidal neurons exhibitconstitutive GABA-independent gating [J]. Mol Pharmacol, 2007,71(2): 539-548.
  • 7Son Y. Molecular mechanisms of general anesthesia [J]. Korean JAnesthesiol, 2010, 59(1): 3-8.
  • 8Thompson AJ, Alqazzaz M, Ulens C,et al. The pharmacologicalprofile of ELIC, a prokaryotic GABA -^ated receptor [J].Neuropharmacology, 2012,63(4): 761-767.
  • 9Nutt DJ, Besson M, Wilson SJ, et al. Blockade of alcohol's amnesticactivity in humans by an alpha5 subtype benzodiazepine receptorinverse agonist[J]. Neuropharmacology, 2007, 53(7) : 810-820.
  • 10Herd MB, Lambert JJ, Belelli D. The general anaesthetic etomidateinhibits the excitability of mouse thalamocortical relay neurons bymodulating multiple modes of GABAa receptor -mediated inhibition[J]. Eur J Neurosci, 2014,40(3): 2487-2501.

二级参考文献19

  • 1Hemmings HC, Akabas MH, Goldstein PA, et al. Emerging molecular mechanisms of general anesthetic action[J]. Trends Pharmacol Sci, 2005, 26(10): 503-510.
  • 2Liu R, Loll PJ, Eckenhoff RG. Structural basis for high-affinity volatile anesthetic binding in a natural 4-helix bundle protein[J]. FASEB J, 2005, 19(6): 567-576.
  • 3Vedula LS, Brannigan G, Economou NJ, et al. A unitary anesthetic binding site at high resolution[J]. J Biol Chem, 2009, 284(36 ) : 24176-24184.
  • 4Nury H, Van Renterghem C, Weng Y, et al. X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel [J]. Nature, 2011, 469(7330): 428-431.
  • 5Guitehounts G, Stewart DS, Forman SA.Two etomidate sites in ct1132")'2 /-aminobutyrie acid type a receptors contribute equally and noneooperatively to modulation of channel gating [ J ]. Anesthesiology, 2012, 116( 6 ) : 1235 -1244.
  • 6Ruesch D, Neumann E, Wulf H, et al. An allosterie eoagonist model for propofol effects on ctl132",/2L /-aminobutyric acid type A receptors[J ]. Anesthesiology, 2012, 116( 1 ) : 47-55.
  • 7Monod J, Wyman J, Changeux JP. On the nature of allosteric transitions: a plausible model[J]. J Mol Biol, 1965, 12(1 ) : 88-118.
  • 8Changeux JP. 50th anniversary of the word "Allosteric"[ J ]. Protein Sei, 2011, 20(7): 1119-1124.
  • 9Yuki K, Astrof NS, Bracken C, et al. The volatile anestheticisoflurane perturbs conformational activa|ion of integrin LFA-1 by binding to the allosterie regulatory cavity[J]. FASEB J, 2008, 22 (12): 4109-4116.
  • 10Yuki K, Bu W, Xi J, et al. Isoflurane binds and stabilizes a closed confirmation of the leukocyte function-associated antigen-I [J]. FASEB J, 2012, 26(11): 4408-4417.

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