[四甲铵衍生物作为不同胆碱酯酶的可逆抑制剂]。

N E Basova, B N Kormilitsyn, A Yu Perchenok, E V Rozengart, V S Saakov, A A Suvorov
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引用次数: 0

摘要

研究四亚甲基双溴铵类化合物的元素有机衍生物对胆碱酯酶(ChE)可逆抑制剂(人红细胞乙酰-ChE、马血清丁基-ChE)抗胆碱酯酶效率的影响。本文研究了西北太平洋不同生境的太平洋鱿鱼(Todarodes pacificus)和大鲵(Berryteuthis magister)个体的视神经节和蛙蛙(Rana temporaria)脑内的胆碱酯(ChE)。双磷抑制剂明显比双铵抑制剂更有效,但这可能与前者的大小和疏水性显著增加有关。有机硅铋铵化合物及其单铵类似物在哺乳动物体内具有同等活性的可逆ChE抑制剂。首先研究了其(苯硫鎓)衍生物,其特点是由于在元素间四亚甲基链中引入氟原子而显著增加疏水性,对哺乳动物ChE也具有显著的抗胆碱酯酶作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[TETRAMETHONIUM DERIVATIVES AS REVERSIBLE INHIBITORS OF DIFFERENT CHOLINESTERASES].

To study the influence of onium atom nature on anticholinesterase efficiency of elementorganic derivatives of tetramethylenbisonium compounds as reversible inhibitors of cholinesterase (ChE) - acetyl-ChE from human erythrocytes, butyryl-ChE from horse serum, ChE from the brain of frog Rana temporaria and ChEs from visual ganglia of Pacific squid Todarodes pacificus and individuals of Comman- der squid Berryteuthis magister from different habitats in the northwestern Pacific Ocean were investigated. Bisphosphonium inhibitors were significantly more potent effectors than bisammonium ones, but this may be associated with a significantly increased size and hydrophobicity of onium groups of the former. Bisammonium organosilicon compound and its monoammonium analogue were equally active reversible ChE inhibitors in mammals. First studied bis(phenyliodonium) derivative, which is characterized by a significant increase in the degree of hydrophobicity due to introduction of fluorine atoms in the interonium tetramethylene chain, also had marked anticholinesterase effects on mammalian ChE.

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