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[有机磷酸胆碱酯酶抑制剂在大脑中的沉积形式]

[Forms of deposition of phosphoorganic cholinesterase inhibitors in the brain].

作者信息

Balashova E K, Pevzner D L, Rozengart V I, Sherstobitov O E, Abduvakhobov A A

出版信息

Vopr Biokhim Mozga. 1975;10:91-6.

PMID:1234672
Abstract

The content and hydrophobic properties (distribution coefficient in hexan : water) of organophosphorus inhibitors OPT of the following structure--R-O (CH3)/P/O/S C2H4SC2H5 have been studied in rat brain. On enlargement of the O-alkyl radical from ethyl to isopropyl and pinacolin hydrophobecity increases from 1 to 12 and 39, while the relative content of the chloroform extractable free OPT in brain, under conditions of uniform distribution, decreases from 11--18% to 3.2%. On incubation of the homogenate at 37 degrees C the further inhibition of the specific cholinesterase of the brain indicates the presence of an absolutely free form of OPT, the amount of which is not dependent on the degree of its hydrophobicity.

摘要

已在大鼠脑中研究了具有以下结构——R - O(CH₃)/P/O/S C₂H₄SC₂H₅的有机磷抑制剂OPT的含量及疏水特性(己烷:水分配系数)。当O - 烷基从乙基增大到异丙基和频哪醇基时,疏水性从1增加到12和39,而在均匀分布条件下,脑中氯仿可萃取的游离OPT的相对含量从11% - 18%降至3.2%。在37℃孵育匀浆时,对脑特异性胆碱酯酶的进一步抑制表明存在绝对游离形式的OPT,其含量不依赖于其疏水程度。

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