胍类毒素对肌肉钠离子通道的电压依赖性阻断作用。
Voltage-dependent blockade of muscle Na+ channels by guanidinium toxins.
作者信息
Moczydlowski E, Hall S, Garber S S, Strichartz G S, Miller C
出版信息
J Gen Physiol. 1984 Nov;84(5):687-704. doi: 10.1085/jgp.84.5.687.
Abstract
Na+ channels from rat muscle plasma membrane vesicles were inserted into neutral planar phospholipid bilayers and were activated by batrachotoxin. Single channel blocking events induced by the addition of various guanidinium toxins were analyzed to derive the rates of channel-toxin association and dissociation. Blocking by tetrodotoxin, saxitoxin, and six natural saxitoxin derivatives containing sulfate or hydroxyl groups were studied. Although the binding affinities vary over 2,000-fold, all of the toxins exhibit identical voltage dependence of the blocking reactions, regardless of the toxin's net charge. The results suggest that the voltage dependence of toxin binding is due to a voltage-dependent conformational equilibrium of the toxin receptor, rather than to direct entry of the charged toxin molecule into the applied transmembrane electric field.
摘要
将来自大鼠肌肉质膜囊泡的钠离子通道插入中性平面磷脂双分子层中，并用蟾毒素激活。分析了添加各种胍类毒素引起的单通道阻断事件，以得出通道 - 毒素结合和解离的速率。研究了河豚毒素、石房蛤毒素以及六种含有硫酸根或羟基的天然石房蛤毒素衍生物的阻断作用。尽管结合亲和力相差超过2000倍，但所有毒素在阻断反应中都表现出相同的电压依赖性，与毒素的净电荷无关。结果表明，毒素结合的电压依赖性是由于毒素受体的电压依赖性构象平衡，而不是带电毒素分子直接进入施加的跨膜电场。
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