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[双吡啶肟作为大鼠骨骼肌中由乙酰胆碱激活的离子通道阻滞剂]

[Dipyroxime as a blocker of ion channels activated by acetylcholine in rat skeletal muscle].

作者信息

Giniatullin R A, Shabunova I A, Nikol'skiĭ E E, Bukharaeva E A

出版信息

Biull Eksp Biol Med. 1987 Jun;103(6):690-2.

PMID:2439141
Abstract

The mechanism of cholinolytic action of dipyroxime--reactivator of the phosphorylated acetylcholinesterase were investigated in the rat diaphragm muscle by voltage-clamp technique. Dipyroxime reduced the amplitude and prolonged the decay of the miniature end-plate currents (MEPC) without affecting its exponential nature. Current-voltage relationship exhibited negative conduction in the hyperpolarized region. Dipyroxime increased the voltage dependence of the time constant of MEPC decay (the membrane potential alteration necessary for e-fold change of the decay time constant reduced from 80 to 35 mV). It was concluded that dipyroxime is a very fast blocker of the open end-plate channels.

摘要

采用电压钳技术在大鼠膈肌上研究了双吡啶肟(磷酸化乙酰胆碱酯酶的重活化剂)的抗胆碱作用机制。双吡啶肟降低了微小终板电流(MEPC)的幅度并延长了其衰减时间,而不影响其指数性质。电流-电压关系在超极化区域呈现负向传导。双吡啶肟增加了MEPC衰减时间常数的电压依赖性(衰减时间常数e倍变化所需的膜电位改变从80 mV降至35 mV)。得出的结论是,双吡啶肟是开放终板通道的非常快速的阻滞剂。

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