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一些具有军事意义的有机磷酸盐和氨基甲酸盐对鳗鱼和兔脑乙酰胆碱酯酶抑制作用的动力学常数。

Kinetic constants for the inhibition of eel and rabbit brain acetylcholinesterase by some organophosphates and carbamates of military significance.

作者信息

Gray P J, Dawson R M

机构信息

Materials Research Laboratories, Defence Science and Technology Organization, Ascot Vale VIC, Australia.

出版信息

Toxicol Appl Pharmacol. 1987 Oct;91(1):140-4. doi: 10.1016/0041-008x(87)90201-8.

Abstract

The kinetics of the inhibition of eel and rabbit brain acetylcholinesterase by a number of organophosphates and carbamates has been studied. Five organophosphates (tabun, sarin, soman, GF, and VX) and two carbamates (neostigmine and physostigmine) were used. Small but significant differences have been found between the two enzyme preparations in both the dissociation constant and the rate constants for the irreversible step. The values of k2 ranged from 0.56 to 1.08 sec-1 for the eel enzyme and 0.19 to 0.73 sec-1 for the rabbit enzyme. Kd varied from 0.3 to 24.5 microM for the eel and 0.3 to 9.3 microM for the rabbit enzyme. The similarity between the enzymes is remarkable considering the differences in the species of origin.

摘要

研究了多种有机磷酸酯和氨基甲酸酯对鳗鱼和兔脑乙酰胆碱酯酶的抑制动力学。使用了五种有机磷酸酯(塔崩、沙林、梭曼、GF和VX)和两种氨基甲酸酯(新斯的明和毒扁豆碱)。在两种酶制剂的解离常数和不可逆步骤的速率常数方面都发现了微小但显著的差异。鳗鱼酶的k2值范围为0.56至1.08秒-1,兔酶的k2值范围为0.19至0.73秒-1。鳗鱼酶的Kd在0.3至24.5微摩尔之间变化,兔酶的Kd在0.3至9.3微摩尔之间变化。考虑到来源物种的差异,这些酶之间的相似性非常显著。

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