Srivastava S, Phadke R S, Govil G
Tata Institute of Fundamental Research, Bombay, India.
Physiol Chem Phys Med NMR. 1987;19(4):241-50.
Physicochemical studies on the binding of etomidate, a fast acting anaesthetic, with lipid bilayers have been carried out. ESR spin labeling studies indicate that the gel to liquid crystalline phase transition of dipalmitoyl phosphatidyl choline (DPPC) vesicles retains its cooperative nature on incorporation of the anaesthetic. For a 5:1 lipid to drug molar ratio, the phase transition occurs at an unusually lower temperature than those observed with other drug-DPPC systems. Results of 13C NMR and 1H NOE experiments suggest that the drug molecules reside in the close proximity of the terminal of hydrocarbon chains of the lipid molecules. 31P NMR and Electron Microscopic experiments indicate that the presence of etomidate alters the normal lamellar structure of DPPC vesicles into hexagonal (HII) type. Based on these observations, a model for drug-lipid binding has been proposed.
已对速效麻醉剂依托咪酯与脂质双层的结合进行了物理化学研究。电子自旋共振（ESR）自旋标记研究表明，二棕榈酰磷脂酰胆碱（DPPC）囊泡从凝胶相到液晶相的转变在加入麻醉剂后仍保持其协同性质。对于脂质与药物摩尔比为5:1的情况，相变发生的温度异常低于其他药物-DPPC系统所观察到的温度。碳-13核磁共振（13C NMR）和质子核Overhauser效应（1H NOE）实验结果表明，药物分子位于脂质分子烃链末端的附近。磷-31核磁共振（31P NMR）和电子显微镜实验表明，依托咪酯的存在将DPPC囊泡的正常层状结构改变为六方（HII）型。基于这些观察结果，提出了一种药物-脂质结合模型。
