溶剂置换作为探究黏液虫通道门控的一种方法。重水对阻塞通道药物动力学特性的影响。
Solvent substitution as a probe of channel gating in Myxicola. Effects of D2O on kinetic properties of drugs that occlude channels.
作者信息
Schauf C L, Bullock J O
出版信息
Biophys J. 1982 Feb;37(2):441-52. doi: 10.1016/S0006-3495(82)84690-0.
Abstract
The effects of solvent substitution on the steady-state and kinetic properties of drugs (gallamine triethiodide) and ions (nonyltriethylammonium and Ba++) known to occlude Na+ and K+ channels have been examined and compared with the effects of D2O on unmodified channels. In general, we observed large isotope effects on the kinetics of occlusion at temperatures of 5 degrees C, but only minor effects at 15 degrees C, consistent with processes involving significant solvent interaction. Steady-state behavior was not affected. In the case of gallamine, where a dual effect on INa is evident, although both processes were D2O sensitive, only the occlusion phase had a significant temperature dependence.
摘要
已研究了溶剂替代对已知可阻断Na+和K+通道的药物（三碘季铵酚）和离子（壬基三乙铵和Ba++）的稳态及动力学特性的影响，并将其与D2O对未修饰通道的影响进行了比较。总体而言，我们观察到在5摄氏度时，溶剂替代对阻断动力学有较大的同位素效应，但在15摄氏度时只有微小效应，这与涉及显著溶剂相互作用的过程一致。稳态行为未受影响。在三碘季铵酚的情况下，对Na电流有明显的双重效应，尽管这两个过程都对D2O敏感，但只有阻断阶段具有显著的温度依赖性。
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