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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.

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。

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