HOW TO ACT LOCAL ANESTHETICS TO SODIUM ION CHANNEL.

从我们最近的研究来看，局部麻醉剂可能通过与神经膜表面结合，抑制钠离子的通过，从而改变通道蛋白的形成，从而诱导其药理作用。本项目采用凝胶层析法和特异超滤法研究了^<14>C -利多卡因对大鼠脑钠通道和神经膜的结合作用。用0.32 M蔗糖，5 mM磷酸钠，pH 7.4, 0.1 mm苯甲磺酰氟，10% (w/v)， 10冲程的电机驱动特氟隆/玻璃均质机对大鼠大脑进行均质。上清液分别在700 g × 10 min、27,000 g × 40 min、120,000 g × 50 min下沉淀。观察钠离子通道分数和神经膜分数与^<14>C -利多卡因和^ 3h - batracho毒素宁（钠通道开启剂）的结合作用。结果表明，^<14 bb0 C -利多卡因和^3H batracho毒素与大鼠脑钠通道没有结合亲和力。超滤法观察到^<14>C -利多卡因与大鼠神经膜的特异性结合亲和力。这些结果再次与我们最近的研究相吻合，局部麻醉剂可能通过与神经膜结合，抑制钠离子的通过，从而改变通道蛋白的形成，从而诱导其药理作用。

From our recent studies, local anesthetics might induce their pharmacological effects by binding to the nerve membrane surface and inhibiting the passage of sodium ion, thereby altering the com formation of channel proteins.This projects were examined the binding effects of ^<14>C -lidocaine to rat brain sodium channel and nerve membrane by using gel chromatography or specific ultra filtration.Rats brain were homogenized in ice-cold 0.32 M sucrose, 5 mM sodium phosphate, pH 7.4, 0.1 mMphenylmethanesulfonyl fluoride, at 10 % (w/v) with 10 strokes of a motor-driven Teflon/ glass homogenizer. The supernatants were sedimented at 700 g × 10 min, 27,000 g × 40 min, 120,000 g × 50 min. Sodium ion channel fraction and nerve membrane fraction were examine the binding effects with ^<14>C -lidocaine and ^3H-batrachotoxinnin (sodium channel opener).The results indicated that there are not seeing the binding affinity of ^<14>C -lidocaine and ^3H batrachotoxinnin with rat brain sodium channel. Specific binding affinity was seen at ^<14>C -lidocaine with rat nerve membrane by using ultra filtration.These results again fits in our recent studies that local anesthetics might induce their pharmacological effects by binding to the nerve membrane and inhibiting the passage of sodium ion, thereby altering the com formation of channel proteins.