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藜芦碱对青蛙骨骼肌钠电流和钙电流的影响。

Effects of veratridine on Na and Ca currents in frog skeletal muscle.

作者信息

Nánási P P, Varró A, Lathrop D A, Bryant S H

机构信息

Department of Physiology, University Medical School of Debrecen, Hungary.

出版信息

Gen Pharmacol. 1994 Dec;25(8):1661-6. doi: 10.1016/0306-3623(94)90369-7.

DOI:10.1016/0306-3623(94)90369-7
PMID:7721043
Abstract
  1. Voltage-clamp experiments were performed to determine the effects of veratridine on Na and Ca currents in frog skeletal muscle fibres. 2. Veratridine (1 microM) did not affect the kinetics of the fast Na current but it did induce a slowly inactivating tetrodotoxin-sensitive inward current that was apparent after Na current inactivation. This slow current had a peak amplitude of 6.7 +/- 0.7 microA/cm2 at -20 mV and decayed monoexponentially with a time constant of 606 +/- 77 ms. 3. The slow current had a voltage-dependence for activation that was similar to that of the fast Na current. Single depolarizing prepulses that induced complete inactivation of the fast Na channels, prevented development of the slow current. Trains of brief depolarizations at increasing frequencies increased the amplitude of the slow current. These results suggest that the slow current may be mediated by veratridine modified Na channels that must be in the open position. 4. The low concentration of veratridine (1 microM) did not affect the Ca current, while 100 microM veratridine reversibly suppressed the Ca current and shifted its peak current-voltage relation towards more negative potentials. Thus, veratridine appears not to be a selective fast Na channel modifier as it may also alter Ca channel gating properties in skeletal muscle fibres.
摘要
  1. 进行电压钳实验以确定藜芦碱对青蛙骨骼肌纤维中钠电流和钙电流的影响。2. 藜芦碱(1微摩尔)不影响快速钠电流的动力学,但它确实诱导了一种缓慢失活的河豚毒素敏感内向电流,该电流在钠电流失活后明显。这种慢电流在-20毫伏时的峰值幅度为6.7±0.7微安/平方厘米,并以606±77毫秒的时间常数单指数衰减。3. 慢电流的激活具有与快速钠电流相似的电压依赖性。诱导快速钠通道完全失活的单个去极化预脉冲可阻止慢电流的产生。频率增加的一系列短暂去极化会增加慢电流的幅度。这些结果表明,慢电流可能由必须处于开放位置的藜芦碱修饰的钠通道介导。4. 低浓度的藜芦碱(1微摩尔)不影响钙电流,而100微摩尔的藜芦碱可逆地抑制钙电流并将其峰值电流-电压关系向更负的电位移动。因此,藜芦碱似乎不是一种选择性的快速钠通道修饰剂,因为它也可能改变骨骼肌纤维中的钙通道门控特性。

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