Sikaris K A, Sawyer W H
Biochem Pharmacol. 1982 Aug 15;31(16):2625-31. doi: 10.1016/0006-2952(82)90709-2.
The preferred position and orientation of two local anaesthetics in lipid bilayers has been determined using fluorescence quenching techniques. The aromatic amine of tetracaine and butesin quenches the fluorescence of a series of n-(9-anthroyloxy) fatty acids (n = 2,6,9,12,16) which place a fluorophore at a graded series of depths from the surface to the centre of a bilayer. A fluorescence method is used to resolve partition coefficients in the transverse plane of the membrane. The results show that the anaesthetics take up a distribution of positions about one or more preferred maxima. The aromatic amine group of tetracaine appears to be buried deep in the bilayer whereas the same group in butesin assumes positions at the surface as well as in the interior of the membrane.
利用荧光猝灭技术确定了两种局部麻醉剂在脂质双分子层中的优选位置和取向。丁卡因和布特辛的芳香胺会猝灭一系列n -（9 - 蒽氧基）脂肪酸（n = 2、6、9、12、16）的荧光，这些脂肪酸将荧光团置于从双分子层表面到中心的一系列渐变深度处。采用荧光方法来解析膜横向平面中的分配系数。结果表明，麻醉剂占据一个或多个优选最大值周围的位置分布。丁卡因的芳香胺基团似乎深埋在双分子层中，而布特辛中的同一基团在膜表面以及内部均占据一定位置。
