HOW TO ACT LOCAL ANESTHETICS TO SODIUM ION CHANNEL.

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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.