Casanovas A M, Labat C, Courriere P, Oustrin J
Biochem Pharmacol. 1985 Mar 1;34(5):663-8. doi: 10.1016/0006-2952(85)90261-8.
The interaction of a series of eight local anaesthetics with cytochrome oxidase chosen as a membrane model protein has been studied with fluorescence technique using quinacrine as a fluorescent probe. The existence of hydrophobic interactions with a non polar region of cytochrome oxidase complex has been shown. The ability of the drug molecules to displace quinacrine bound to cytochrome oxidase correlate as closely with their anaesthetic potency as with their octanol-water partition coefficient. Our results are in good agreement with a recent model of local anaesthetic action on nerve membranes presenting a site of anaesthesia including both lipid binding and protein binding environments.
使用喹吖因作为荧光探针,采用荧光技术研究了一系列八种局部麻醉剂与作为膜模型蛋白的细胞色素氧化酶之间的相互作用。已证明存在与细胞色素氧化酶复合物非极性区域的疏水相互作用。药物分子取代与细胞色素氧化酶结合的喹吖因的能力,与其麻醉效力的相关性与它们的辛醇 - 水分配系数的相关性一样密切。我们的结果与最近提出的局部麻醉剂对神经膜作用的模型高度一致,该模型提出了一个包括脂质结合和蛋白质结合环境的麻醉位点。