水合氯醛和三氯乙醇对乙醇脱氢酶的抑制作用：在水合氯醛 - 乙醇相互作用中的可能作用。

Inhibition of alcohol dehydrogenase by chloral hydrate and trichloroethanol: possible role in the chloral hydrate-ethanol interaction.

作者信息

Sharkawi M, De Saint Blanquat G, Elfassy B

出版信息

Toxicol Lett. 1983 Jul;17(3-4):321-8. doi: 10.1016/0378-4274(83)90245-x.

Abstract

Both chloral hydrate and trichloroethanol inhibited mouse liver alcohol dehydrogenase (LADH) in vitro. The inhibition of LADH by chloral hydrate appears to be non-competitive in nature with an inhibition constant (Ki) of about 2.7 X 10(-4) M. The inhibition of LADH by trichloroethanol was competitive and the (Ki) was about 2.7 X 10(-5) M. The elimination of ethanol from the blood and brain was significantly reduced in chloral hydrate- or trichloroethanol-pretreated mice. Since reduced elimination of ethanol could result in the prolongation of its central depressant activity, we suggest that this should be considered as a factor in the enhanced pharmacological effects of ethanol-chloral hydrate mixtures.

摘要

水合氯醛和三氯乙醇在体外均能抑制小鼠肝脏乙醇脱氢酶（LADH）。水合氯醛对LADH的抑制作用在本质上似乎是非竞争性的，抑制常数（Ki）约为2.7×10⁻⁴M。三氯乙醇对LADH的抑制作用是竞争性的，Ki约为2.7×10⁻⁵M。在经水合氯醛或三氯乙醇预处理的小鼠中，血液和大脑中乙醇的清除率显著降低。由于乙醇清除率降低可能导致其中枢抑制活性延长，我们认为这应被视为乙醇 - 水合氯醛混合物药理作用增强的一个因素。