Kostyuk P G, Molokanova E A, Pronchuk N F, Savchenko A N, Verkhratsky A N
Department of General Physiology of the Nervous System, A.A. Bogomoletz Institute of Physiology, Kiev, Ukraine.
Neuroscience. 1992 Dec;51(4):755-8. doi: 10.1016/0306-4522(92)90515-4.
The effects of ethosuximide on calcium channels were studied on dorsal root ganglion neurons from one-day-old rats using the patch-clamp technique. Bath application of ethosuximide induced dose-dependent and reversible suppression of calcium currents without affecting their time-course. Substantial differences between the effects of ethosuximide on the low-threshold and high-threshold (T- and L-) currents were observed. Ethosuximide reduced the T-current with greater potency than the L-current (Kd for T-current is 7 microM vs 15 microM for L-current). This relative specificity of its action still remained if applied at concentrations up to 1 mM. These data support the hypothesis according to which the anti-epileptic action of ethosuximide is related to reduction of the low-threshold calcium currents in sensory neurons.
采用膜片钳技术,研究了乙琥胺对1日龄大鼠背根神经节神经元钙通道的影响。浴槽给药乙琥胺可引起钙电流剂量依赖性和可逆性抑制,且不影响其时程。观察到乙琥胺对低阈值和高阈值(T型和L型)电流的影响存在显著差异。乙琥胺降低T型电流的效力大于L型电流(T型电流的Kd为7 microM,L型电流为15 microM)。即使在高达1 mM的浓度下应用,其作用的这种相对特异性仍然存在。这些数据支持了这样一种假说,即乙琥胺的抗癫痫作用与感觉神经元中低阈值钙电流的减少有关。