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二异丙基氟磷酸酯:对胆碱能受体离子电导的抑制作用。

Diisopropylfluorophosphate: suppression of ionic conductance of the cholinergic receptor.

作者信息

Kuba K, Albuquerque E X, Barnard E A

出版信息

Science. 1973 Aug 31;181(4102):853-6. doi: 10.1126/science.181.4102.853.

DOI:10.1126/science.181.4102.853
PMID:4724073
Abstract

When frog sartorius muscles were exposed to diisopropylfluorophosphate, the amplitude and half-decay time of the end-plate current decreased; the half-decay time became almost potential-independent and the equilibrium potential for the end-plate current was more negative than during control conditions. When the excess reagent was removed by washing so that only the phosphorylated acetylcholinesterase remained, the amplitude of the end-plate current was restored, while its half-decay time was markedly increased. These findings reveal that this organophosphate significantly affects the receptor-ionic conductance modulator complex in addition to its well-known anticholinesterase activity.

摘要

当青蛙的缝匠肌暴露于二异丙基氟磷酸时,终板电流的幅度和半衰期降低;半衰期几乎变得与电位无关,且终板电流的平衡电位比对照条件下更负。当通过冲洗去除过量试剂,使得仅留下磷酸化的乙酰胆碱酯酶时,终板电流的幅度得以恢复,而其半衰期则显著增加。这些发现表明,这种有机磷酸酯除了具有其众所周知的抗胆碱酯酶活性外,还会显著影响受体 - 离子电导调节复合物。

相似文献

1
Diisopropylfluorophosphate: suppression of ionic conductance of the cholinergic receptor.二异丙基氟磷酸酯:对胆碱能受体离子电导的抑制作用。
Science. 1973 Aug 31;181(4102):853-6. doi: 10.1126/science.181.4102.853.
2
A study of the irreversible cholinesterase inhibitor, diisopropylfluorophosphate, on time course of end-plate currents in frog sartorius muscle.一项关于不可逆胆碱酯酶抑制剂二异丙基氟磷酸酯对青蛙缝匠肌终板电流时间进程影响的研究。
J Pharmacol Exp Ther. 1974 May;189(2):499-512.
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Effect of histrionicotoxin on the ionic conductance modulator of the cholinergic receptor: a quantitative analysis of the end-plate current.组胺毒素对胆碱能受体离子电导调节剂的作用:终板电流的定量分析
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Amantadine: neuromuscular blockade by suppression of ionic conductance of the acetylcholine receptor.金刚烷胺:通过抑制乙酰胆碱受体的离子电导实现神经肌肉阻滞。
Science. 1978 Feb 17;199(4330):788-90. doi: 10.1126/science.622570.
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Meproadifen reaction with the ionic channel of the acetylcholine receptor: potentiation of agonist-induced desensitization at the frog neuromuscular junction.美普罗地芬与乙酰胆碱受体离子通道的反应:增强青蛙神经肌肉接头处激动剂诱导的脱敏作用。
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Pflugers Arch. 1984 May;401(1):84-90. doi: 10.1007/BF00581537.
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