Local anesthetic-phospholipid interactions. The pH dependence of the binding of dibucaine to dimyristoylphosphatidylcholine vesicles.
Local anesthetic-phospholipid interactions. The pH dependence of the binding of dibucaine to dimyristoylphosphatidylcholine vesicles.
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局部麻醉剂-磷脂相互作用。
DOI：
10.1016/0005-2736(85)90354-2
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发表时间：
1985
期刊：
影响因子：
--
通讯作者：
Mahin D. Ghahramani
中科院分区：
文献类型：
--
作者：
M. Eftink;Ravinder K. Puri;Mahin D. Ghahramani
用平衡透析法研究了局麻药二布卡因与二myristoyl磷脂酰胆碱单层囊泡的相互作用。结果表明，当pH值从5.0增加到7.5时，二布卡因的饱和结合谱为1.26·103m -1 ~ 2.57·103m -1。在每个ph值下，组成一个结合位点的磷脂分子数约为5个。对数据的分析也使用了Stern模型，该模型考虑了由于表面电位的积累而对阳离子药物结合的静电效应。
The interaction of the local anesthetic dibucaine with unilamellar vesicles of dimyristoylphosphatidylcholine was studied by equilibrium dialysis. Saturating binding profiles (as a function of dibucaine) were found, with apparent association constant ranging from 1.26·103M-1to 2.57·103M-1as pH is increased from 5.0 to 7.5. The number of phospholipid molecules comprising a binding site was found to be about 5 at each pH. Analysis of the data was also achieved using the Stern model, which takes into account the electrostatic effect on binding of the cationic drug due to the build up of a surface potential.