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R,S-沙丁胺醇对豚鼠慢肌和快肌不完全强直收缩的对映体效应。

Effects of the enantiomers of R,S-salbutamol on incompletely fused tetanic contractions of slow- and fast-twitch skeletal muscles of the guinea-pig.

作者信息

Prior C, Leonard M B, McCullough J R

机构信息

Department of Physiology and Pharmacology, University of Strathclyde, Glasgow, Scotland.

出版信息

Br J Pharmacol. 1998 Feb;123(3):558-64. doi: 10.1038/sj.bjp.0701627.

Abstract
  1. The effects of racemic R,S-salbutamol, and its individual enantiomers have been studied on incompletely fused (sub-tetanic) contractile responses of fast- and slow-contracting isolated skeletal muscles of the guinea-pig. 2. R,S-salbutamol (2-4 microM) decreased the peak force of sub-tetani in the slow-contracting soleus muscle and increased the peak force of sub-tetani in the fast-contracting peroneus longus muscle. It also increased the force of the first twitch of sub-tetani in both muscles. The decrease in the peak force of sub-tetani in the soleus muscle was due to defusion of the individual twitches caused by a shortening of their time course. 3. The effects of 4 microM of the racemate on both fast- and slow-contracting muscles were mimicked by 2 microM R-salbutamol (levalbuterol). However, 2 microM S-salbutamol was devoid of activity in both muscles. 4. We concluded that all the effects of R,S-salbutamol on guinea-pig skeletal muscles are due to the activity of the R-enantiomer. Thus there is a common enantiomeric profile for the skeletal muscle and bronchorelaxant activity of the compound.
摘要
  1. 研究了消旋R,S-沙丁胺醇及其单个对映体对豚鼠快速收缩和慢速收缩的离体骨骼肌不完全融合(亚强直)收缩反应的影响。2. R,S-沙丁胺醇(2 - 4微摩尔)降低了慢速收缩的比目鱼肌中亚强直收缩的峰值力,并增加了快速收缩的腓骨长肌中亚强直收缩的峰值力。它还增加了两块肌肉中亚强直收缩的第一次抽搐的力量。比目鱼肌中亚强直收缩峰值力的降低是由于单个抽搐的时间进程缩短导致的融合减少。3. 4微摩尔外消旋体对快速和慢速收缩肌肉的作用可被2微摩尔R-沙丁胺醇(左旋沙丁胺醇)模拟。然而,2微摩尔S-沙丁胺醇在两块肌肉中均无活性。4. 我们得出结论,R,S-沙丁胺醇对豚鼠骨骼肌的所有作用均归因于R-对映体的活性。因此,该化合物的骨骼肌和支气管舒张活性具有共同的对映体特征。

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