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氟烷可缩短乙酰胆碱受体通道动力学过程,而不影响其电导率。

Halothane shortens acetylcholine receptor channel kinetics without affecting conductance.

作者信息

Lechleiter J, Gruener R

出版信息

Proc Natl Acad Sci U S A. 1984 May;81(9):2929-33. doi: 10.1073/pnas.81.9.2929.

DOI:10.1073/pnas.81.9.2929
PMID:6326154
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC345187/
Abstract

The extracellular patch-clamp technique was used to examine how halothane, a general anesthetic, affects the properties of single nicotinic acetylcholine receptor channels of embryonic Xenopus skeletal muscle cells grown in culture. Under control conditions, single-channel events showed a bimodal distribution on the basis of current amplitudes. This distribution was maintained during exposure to halothane and its washout. In addition, the mean current value of the low-and high-amplitude channels was unaffected by the presence of the anesthetic at clinically relevant concentrations. In contrast, halothane shortened the burst durations of both channel types in a concentration-dependent manner. This shortening of burst durations may be an expression of the more rapid relaxation of the channel protein to the nonconducting state, possibly due to the disordering effect of the anesthetic on membrane lipids in which the receptor protein is embedded. This functional change, in the behavior of the synaptic receptor, provides further direct information on the mode of action of general anesthetics.

摘要

采用细胞外膜片钳技术,研究了全身麻醉药氟烷对培养的非洲爪蟾胚胎骨骼肌细胞单个烟碱型乙酰胆碱受体通道特性的影响。在对照条件下,单通道事件在电流幅度的基础上呈现双峰分布。在接触氟烷及其洗脱过程中,这种分布得以维持。此外,低幅度和高幅度通道的平均电流值不受临床相关浓度麻醉药的影响。相比之下,氟烷以浓度依赖的方式缩短了两种通道类型的爆发持续时间。爆发持续时间的缩短可能是通道蛋白更快松弛到非传导状态的一种表现,这可能是由于麻醉药对嵌入受体蛋白的膜脂质的紊乱作用。突触受体行为的这种功能变化,为全身麻醉药的作用方式提供了进一步的直接信息。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30db/345187/e21a8f161d4d/pnas00610-0338-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30db/345187/e21a8f161d4d/pnas00610-0338-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30db/345187/e21a8f161d4d/pnas00610-0338-a.jpg

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本文引用的文献

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Mechanisms of anaesthesia: a review.麻醉机制:综述
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The effects of some inhalation anaesthetics on the sodium current of the squid giant axon.某些吸入麻醉剂对乌贼巨大轴突钠电流的影响。
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Acetylcholine receptor kinetics. A description from single-channel currents at snake neuromuscular junctions.乙酰胆碱受体动力学。来自蛇神经肌肉接头单通道电流的描述。
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