Cohen I S, Strichartz G R
Biophys J. 1977 Mar;17(3):275-9. doi: 10.1016/S0006-3495(77)85656-7.
The use of the maximum rate-of-rise of the action potential (Vmax) as a measure of the sodium conductance in excitable membranes is invalid. In the case of membrane action potentials, Vmax depends on the total ionic current across the membrane; drugs or conditions that alter the potassium or leak conductances will also affect Vmax. Likewise, long-term depolarization of the membrane lessens the fraction of total ionic current that passes through the sodium channels by increasing potassium conductance and inactivating the sodium conductance, and thereby reduces the effect of Vmax of drugs that specifically block sodium channels. The resultant artifact, an apparent voltage-dependent potency of such drugs, is theoretically simulated for the effects of tetrodotoxin on the Hodgkin-Huxley squid axon.
将动作电位的最大上升速率(Vmax)用作可兴奋膜中钠电导的量度是无效的。就膜动作电位而言,Vmax取决于跨膜的总离子电流;改变钾电导或漏电导的药物或条件也会影响Vmax。同样,膜的长期去极化会通过增加钾电导和使钠电导失活来减少通过钠通道的总离子电流的比例,从而降低特异性阻断钠通道的药物对Vmax的影响。由此产生的假象,即此类药物明显的电压依赖性效力,在理论上针对河豚毒素对霍奇金-赫胥黎鱿鱼轴突的影响进行了模拟。