Molnár P, Erdö S L
CNS Pharmacology Laboratory, Chinoin Co. Ltd., Budapest, Hungary.
Eur J Pharmacol. 1995 Feb 6;273(3):303-6. doi: 10.1016/0014-2999(94)00755-v.
The effects of vinpocetine and phenytoin on voltage-gated Na+ channels were examined on cultured cerebrocortical neurones of the rat using a conventional whole-cell patch-clamp method. Vinpocetine and phenytoin decreased Na+ currents in a concentration-dependent manner, with IC50 values of 44.2 +/- 14.6 and 50.5 +/- 17.4 microM, respectively. Both compounds shifted the voltage dependence of the steady-state inactivation of the channel in the hyperpolarising direction. This pronounced Na+ channel blocking activity may contribute to the neuroprotective and anticonvulsant effects of vinpocetine.
采用传统的全细胞膜片钳方法，在大鼠培养的大脑皮质神经元上研究了长春西汀和苯妥英对电压门控性钠通道的作用。长春西汀和苯妥英均以浓度依赖性方式降低钠电流，IC50值分别为44.2±14.6和50.5±17.4微摩尔。两种化合物均使通道稳态失活的电压依赖性向超极化方向移动。这种明显的钠通道阻断活性可能有助于长春西汀的神经保护和抗惊厥作用。
