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Biophys J. 1990 Jan;57(1):147-52. doi: 10.1016/S0006-3495(90)82515-7.
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Molecular requisites for drug binding to muscle CLC-1 and renal CLC-K channel revealed by the use of phenoxy-alkyl derivatives of 2-(p-chlorophenoxy)propionic acid.使用2-(对氯苯氧基)丙酸的苯氧基烷基衍生物揭示药物与肌肉CLC-1和肾脏CLC-K通道结合的分子要求。
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本文引用的文献

1
THE EFFECTS OF ANIONS ON EXCITABLE CELLS.阴离子对可兴奋细胞的影响。
Pharmacol Rev. 1964 Jun;16:193-221.
2
Perchlorate-induced alterations in electrical and mechanical parameters of frog skeletal muscle fibres.高氯酸盐引起的青蛙骨骼肌纤维电学和力学参数的改变。
J Physiol. 1983 Oct;343:197-214. doi: 10.1113/jphysiol.1983.sp014888.
3
How perchlorate improves excitation-contraction coupling in skeletal muscle fibers.高氯酸盐如何改善骨骼肌纤维中的兴奋-收缩偶联。
Biophys J. 1983 Aug;43(2):247-9. doi: 10.1016/S0006-3495(83)84346-X.
4
Actions of some anions on electrical properties and mechanical threshold of frog twitch muscle.某些阴离子对青蛙抽动肌肉电特性和机械阈值的作用。
J Physiol. 1968 Sep;198(2):291-309. doi: 10.1113/jphysiol.1968.sp008607.
5
The kinetics of mechanical activation in frog muscle.青蛙肌肉中机械激活的动力学。
J Physiol. 1969 Sep;204(1):207-30. doi: 10.1113/jphysiol.1969.sp008909.
6
Excitation-contraction coupling in skeletal muscle.骨骼肌中的兴奋-收缩偶联
Pharmacol Rev. 1965 Sep;17(3):265-320.
7
Chloride conductance in normal and myotonic muscle fibres and the action of monocarboxylic aromatic acids.正常及强直性肌纤维中的氯电导和单羧基芳香酸的作用
J Physiol. 1971 Dec;219(2):367-83. doi: 10.1113/jphysiol.1971.sp009667.
8
Internal citrate ions reduce the membrane potential for contraction threshold in mammalian skeletal muscle fibers.细胞内的柠檬酸根离子可降低哺乳动物骨骼肌纤维收缩阈值的膜电位。
Biophys J. 1988 Apr;53(4):609-16. doi: 10.1016/S0006-3495(88)83139-4.
9
Effects of guanidinium on EC coupling and tension generation in frog skeletal muscle.胍盐对青蛙骨骼肌兴奋-收缩偶联及张力产生的影响。
J Muscle Res Cell Motil. 1988 Dec;9(6):541-51. doi: 10.1007/BF01738759.
10
The differential effects of twitch potentiators on charge movements in frog skeletal muscle.强直收缩增强剂对青蛙骨骼肌电荷移动的不同作用。
J Physiol. 1986 Nov;380:17-33. doi: 10.1113/jphysiol.1986.sp016269.

手性苯氧基羧酸对青蛙骨骼肌兴奋-收缩偶联的对映体效应。

Enantiomeric effects on excitation-contraction coupling in frog skeletal muscle by a chiral phenoxy carboxylic acid.

作者信息

Heiny J A, Jong D, Bryant S H, Conte-Camerino D, Tortorella V

机构信息

Department of Physiology and Biophysics, University of Cincinnati, Ohio 45267-0576.

出版信息

Biophys J. 1990 Jan;57(1):147-52. doi: 10.1016/S0006-3495(90)82515-7.

DOI:10.1016/S0006-3495(90)82515-7
PMID:2297560
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1280651/
Abstract

Aromatic monocarboxylic acids are known to significantly potentiate the mechanical response of skeletal muscle fibers. In this study we investigated the effects of enantiomers of 2-(4-chlorophenoxy)propionic acid, chemically one of the simplest aromatic monocarboxylic acids with chiral properties, on mechanical threshold and charge movement in frog skeletal muscle. The R(+), but not the S(-), enantiomer lowered rheobase mechanical threshold and shifted charge movement to more negative potentials. The R(+) enantiomer also significantly slowed charge movement kinetics, with pronounced delays of the OFF charge transitions. These effects required high temperature for their production. The stereospecific actions of the R(+) enantiomer are interpreted in terms of a specific interaction of this compound at an anion-sensitive site involved in excitation-contraction coupling, most likely on the dihydropryidine-sensitive voltage sensor in the T-system.

摘要

已知芳香族一元羧酸能显著增强骨骼肌纤维的机械反应。在本研究中,我们研究了2-(4-氯苯氧基)丙酸(化学上是最简单的具有手性性质的芳香族一元羧酸之一)的对映体对青蛙骨骼肌机械阈值和电荷移动的影响。R(+)对映体而非S(-)对映体降低了基强度机械阈值,并使电荷移动向更负的电位偏移。R(+)对映体还显著减慢了电荷移动动力学,OFF电荷转变有明显延迟。这些效应需要高温才能产生。R(+)对映体的立体特异性作用可通过该化合物在参与兴奋-收缩偶联的阴离子敏感位点上的特异性相互作用来解释,最有可能是在T系统中对二氢吡啶敏感的电压传感器上。