Changes of acetylcholinesterase activity in various parts of brain following nontreated and treated soman poisoning in rats.

J Kassa, J Bajgar
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引用次数: 16

Abstract

Changes of acetylcholinesterase (AChE) activity in various parts of the brain (frontal cortex, medulla oblongata, pons Varoli, cerebellum, hypothalamus, and hippocampus), following im sublethal non-treated and treated soman poisoning were studied. As a treatment, two antidotal mixtures containing atropine and either obidoxime or oxime HI-6 were used. This antidotal treatment was administered im for 30 s following soman intoxication. The AChE activities in the various brain tissues were evaluated at 1 and 3 h following soman administration. As expected, the highly toxic organophosphorus compound, soman, markedly inhibited AChE activity in all the brain sections at both time intervals. Both oximes had little influence on soman-induced AChE inhibition, but only the HI-6 mixture was able to reactivate soman-inhibited AChE significantly in some of the brain parts (frontal cortex, pons Varoli, hypothalamus). In the brain, the effect of HI-6 against soman-induced AChE inhibition is higher in comparison with obidoxime, but not quite satisfactory. Despite its limited effectiveness in the brain, HI-6 seems to be the most effective oxime yet found against soman poisoning because of its high reactivating effect in the peripheral compartment and other beneficial effects.

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大鼠脑各部位乙酰胆碱酯酶活性的变化。
研究了未治疗和治疗的人体中毒亚致死期大鼠大脑各部位(额叶皮质、延髓、脑桥、小脑、下丘脑和海马)乙酰胆碱酯酶(AChE)活性的变化。作为治疗,使用两种含有阿托品和奥比肟或肟HI-6的解毒剂混合物。这种解毒治疗在人体中毒后持续30秒。在给药后1、3小时,测定各组脑组织乙酰胆碱酯酶活性。正如预期的那样,剧毒的有机磷化合物索曼在两个时间间隔内显著抑制了所有脑切片的乙酰胆碱酯酶活性。两种肟对索曼诱导的AChE抑制作用影响不大,但只有HI-6混合物能够在大脑的某些部位(额叶皮质、脑桥、下丘脑)显著地重新激活索曼抑制的AChE。在大脑中,与奥比多肟相比,HI-6对soman诱导的AChE抑制的作用更高,但并不十分令人满意。尽管其在大脑中的有效性有限,但HI-6似乎是迄今为止发现的对抗人体中毒最有效的肟,因为它在外周腔室中具有高度的再激活作用和其他有益作用。
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