Giniatullin R A, Shabunova I A, Nikol'skiĭ E N, Bukharaeva E A
Neirofiziologiia. 1988;20(3):351-7.
Reactivating (RA) and cholinolytic (Chl) effects of dipyroxime in soleus and diaphragm muscles of the rat were estimated by amplitudes and durations of miniature end-plate potentials (MEPP) and currents (MEPC). After armin-induced inhibition of acetylcholinesterase (AchE), the action of dipyroxime in concentrations of 5.10(-6)-5.10(-4) mol/l on the amplitude and duration of MEPPs and MEPCs represents the combination of RA and Chl effects. Separate study of the RA effect (after washing out of the reactivator) has shown that this effect increased within the whole range of concentrations used. Complete reactivation of phosphorylated AchE was achieved at dipyroxime concentrations of 2-5.10(-4) mol/l. Separate analysis of Chl effect (in voltage-clamp experiments with intact AchE) has shown that dipyroxime suppressed acetylcholine-induced responses due to a block of cholinoreceptors in the open conformation. This block was characterized by prolongation of MEPCs decay without affecting its exponential nature. It is concluded that dipyroxime is a "very fast blocker".
通过微小终板电位（MEPP）和电流（MEPC）的幅度和持续时间，评估了双吡啶肟对大鼠比目鱼肌和膈肌的重活化（RA）及胆碱能解聚（Chl）作用。在阿米林诱导乙酰胆碱酯酶（AchE）抑制后，浓度为5×10⁻⁶ - 5×10⁻⁴ mol/L的双吡啶肟对MEPP和MEPC幅度及持续时间的作用代表了RA和Chl作用的组合。对RA作用的单独研究（在洗去重活化剂后）表明，在所使用的整个浓度范围内该作用均增强。在双吡啶肟浓度为2 - 5×10⁻⁴ mol/L时实现了磷酸化AchE的完全重活化。对Chl作用的单独分析（在完整AchE的电压钳实验中）表明，双吡啶肟抑制了乙酰胆碱诱导的反应，这是由于其对处于开放构象的胆碱能受体的阻断。这种阻断的特征是MEPC衰减延长，但不影响其指数性质。得出的结论是，双吡啶肟是一种“非常快速的阻断剂”。
