The neuronal lipid membrane permeability was markedly increased by bupivacaine and mildly affected by lidocaine and ropivacaine
The neuronal lipid membrane permeability was markedly increased by bupivacaine and mildly affected by lidocaine and ropivacaine
复制标题
DOI：
10.1016/s0014-2999(02)02555-4
复制
发表时间：
2002-11-29
影响因子：
5
通讯作者：
Recio-Pinto, E
中科院分区：
文献类型：
--
作者：
Pardo, L;Blanck, TJJ;Recio-Pinto, E
我们研究了局部麻醉剂对离子膜电导（膜电导）的作用和在胆固醇存在和不存在下与神经元磷脂形成的膜的选择性。在不含胆固醇的膜中，1 mM布比卡因和罗哌卡因使膜电导增加了4.5倍; 5 mM利多卡因、罗哌卡因和布比卡因分别使膜电导增加了2.7倍、2.8倍和22.2倍。在胆固醇的存在下，5 mM罗哌卡因没有影响，利多卡因降低膜电导率2倍，布比卡因增加膜电导率17倍。局部麻醉剂不影响膜中的离子选择性没有胆固醇，但他们都降低了膜中的Na+选择性与胆固醇。胆固醇通过消除或逆转Na+电导增加和降低Cl-电导增加来降低利多卡因和罗哌卡因诱导的膜电导增加。在没有胆固醇的情况下，5 mM布比卡因增加Na+电导（38倍）和Cl-电导（19倍），而在胆固醇的存在下，它只增加Cl-电导（26倍）。在所研究的局部麻醉剂中，罗哌卡因的膜毒性最小，而布比卡因的毒性最大。(C)2002 Elsevier Science B. V.保留所有权利。
We investigated the local anesthetic action on ionic membrane conductance (membrane conductance) and selectivity in membranes formed with neuronal phospholipids in the absence and presence of cholesterol. In membranes without cholesterol, 1 MM bupivacaine and ropivacaine increased the membrane conductance similar to 4.5-fold; and 5 mM lidocaine, ropivacaine and bupivacaine increased the membrane conductance by 2.7-, 2.8- and 22.2-fold, respectively. In the presence of cholesterol, 5 mM ropivacaine had no effect, lidocaine decreased the membrane conductance by 2-fold, and bupivacaine increased the membrane conductance by 17-fold. Local anesthetics did not affect the ion selectivity in membranes without cholesterol, but they all decreased the Na+ selectivity in membranes with cholesterol. Cholesterol reduced the lidocaine- and ropivacaine-induced membrane conductance increase by eliminating or reversing the Na+ conductance increase and by lowering the Cl- conductance increase. In the absence of cholesterol, 5 mM bupivacaine increased both Na+ conductance (38-fold) and Cl- conductance (19-fold), while in the presence of cholesterol it only increased Cl- conductance (26-fold). Of the local anesthetics studied, ropivacaine was the least membrane toxic while bupivacaine was the most toxic. (C) 2002 Elsevier Science B.V. All rights reserved.