Mazzanti L, Pastuszko A, Lenaz G
Biochim Biophys Acta. 1986 Sep 25;861(1):105-10. doi: 10.1016/0005-2736(86)90376-7.
This investigation shows that the effects of general anesthetics previously observed in vitro on membrane fluidity and on enzymic activities and occurring at concentrations calculated to be clinically relevant can be reproduced in vivo in anesthetized animals. Anesthesia with 2-chlorophenyl-2-methylaminocyclohexanone (ketamine) induces a more fluid state of rat-brain synaptic and mitochondrial membranes, as shown by the rotational correlation times of the spin labels 16-doxylstearate and 5-doxylstearate. Changes in acetylcholinesterase activity, with a decrease in Vmax and no change in the Km for acetylcholine, closely follow the fluidity increase.
本研究表明,先前在体外观察到的全身麻醉药对膜流动性和酶活性的影响,以及在计算得出的临床相关浓度下出现的这些影响,可在麻醉动物体内重现。用2-氯苯基-2-甲氨基环己酮(氯胺酮)麻醉可诱导大鼠脑突触膜和线粒体膜呈现更具流动性的状态,这由自旋标记物16-脱氧硬脂酸酯和5-脱氧硬脂酸酯的旋转相关时间表明。乙酰胆碱酯酶活性的变化,表现为Vmax降低而乙酰胆碱的Km不变,与流动性增加密切相关。