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吡啶斯的明对梭曼所致神经肌肉阻滞的逆转作用。

The reversal by pyridostigmine of neuromuscular block produced by soman.

作者信息

French M C, Wetherell J R, White P D

出版信息

J Pharm Pharmacol. 1979 May;31(5):290-4. doi: 10.1111/j.2042-7158.1979.tb13503.x.

Abstract

The effect of pyridostigmine on neuromuscular block produced by soman was studied in the isolated phrenic nerve-diaphragm preparation. In the rat, soman produced an irreversible reduction in tetanic tension and functional acetylcholinesterase (AChE) activity. Pretreatment with pyridostigmine before exposure of the diaphragm to soman, followed by removal of the anticholinesterase from the organ bath, produced a return of tetanic tension and an increase of 5% in functional AChE activity. Similar results were obtained in the guinea-pig. The changes in synaptic AChE activity were verified pharmacologically by showing a decrease in the blocking activity of acetylcholine in preparations pretreated with pyridostigmine in comparison to those given soman alone following removal of the anti-cholinesterase. The blocking dose of carbachol did not change in these two groups indicating that desensitization was not a component of the protective action. A comparison was also made of the results obtained by measuring inhibition of AChE in situ with those obtained from muscle homogenates. The implications of these results are discussed.

摘要

在离体膈神经 - 膈肌标本中研究了吡啶斯的明对梭曼所致神经肌肉阻滞的影响。在大鼠中,梭曼使强直张力和功能性乙酰胆碱酯酶(AChE)活性出现不可逆降低。在膈肌暴露于梭曼之前用吡啶斯的明预处理,然后从器官浴中去除抗胆碱酯酶,强直张力恢复,功能性AChE活性增加5%。在豚鼠中也得到了类似结果。通过显示与单独给予梭曼后去除抗胆碱酯酶的标本相比,用吡啶斯的明预处理的标本中乙酰胆碱的阻断活性降低,从药理学上证实了突触AChE活性的变化。这两组中卡巴胆碱的阻断剂量没有变化,表明脱敏不是保护作用的组成部分。还对通过原位测量AChE抑制获得的结果与从肌肉匀浆获得的结果进行了比较。讨论了这些结果的意义。

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