Ondrias K, Misík V, Stolc S
Drugs Exp Clin Res. 1986;12(9-10):837-40.
Local anaesthetic carbisocaine decreased the electrical conductivity of gramicidin channels in planar lipid membrane made from bovine brain total lipids in n-hexane at the concentration (1.6 +/- 1.3) X 10(-5) mol/l, which is similar to that found to block propagation of action potential on the sciatic nerve. To study the mechanism of this effect the authors investigated the disordering effect of carbisocaine on rat total lipid membranes at the 5th, 12th and the 16th carbon membrane depths, using ESR spectroscopy of spin-labelled stearic acids. Carbisocaine disorders the membrane and the effect increases towards the methyl terminal of the lipid acyl chains. It is suggested that carbisocaine-induced perturbation of the membrane may have a secondary influence on the conductivity of gramicidin channels in the membrane.
局部麻醉药卡比佐卡因在正己烷中由牛脑总脂质制成的平面脂质膜中，以(1.6±1.3)×10⁻⁵mol/l的浓度降低了短杆菌肽通道的电导率，这一浓度与在坐骨神经上阻断动作电位传播的浓度相似。为研究这种作用机制，作者利用自旋标记硬脂酸的电子自旋共振光谱法，研究了卡比佐卡因在第5、12和16个碳膜深度对大鼠总脂质膜的无序化作用。卡比佐卡因使膜无序化，且这种作用朝着脂质酰基链的甲基末端增强。提示卡比佐卡因引起的膜扰动可能对膜中短杆菌肽通道的电导率产生继发性影响。
