A Comparison of the Neuroprotective and Reactivating Efficacy of a Novel Bispyridinium Oxime K870 with Commonly Used Pralidoxime and the Oxime HI-6 in Tabun-Poisoned Rats.

Q3 Medicine
Jiří Kassa, Jana Hatlapatková, Jana Žďárová Karasová, Vendula Hepnarová, Filip Caisberger, Jaroslav Pejchal
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Abstract

Aim: The comparison of neuroprotective and central reactivating effects of the oxime K870 in combination with atropine with the efficacy of standard antidotal treatment in tabun-poisoned rats.

Methods: The neuroprotective effects of antidotal treatment were determined in rats poisoned with tabun at a sublethal dose using a functional observational battery 2 h and 24 h after tabun administration, the tabun-induced brain damage was investigated by the histopathological evaluation and central reactivating effects of oximes was evaluated by the determination of acetylcholinesterase activity in the brain using a standard spectrophotometric method.

Results: The central reactivating efficacy of a newly developed oxime K870 roughly corresponds to the central reactivating efficacy of pralidoxime while the ability of the oxime HI-6 to reactivate tabun-inhibited acetylcholinesterase in the brain was negligible. The ability of the oxime K870 to decrease tabun-induced acute neurotoxicity was slightly higher than that of pralidoxime and similar to the oxime HI-6. These results roughly correspond to the histopathological evaluation of tabun-induced brain damage.

Conclusion: The newly synthesized oxime K870 is not a suitable replacement for commonly used oximes in the antidotal treatment of acute tabun poisonings because its neuroprotective efficacy is only slightly higher or similar compared to studied currently used oximes.

新型双吡啶肟K870与常用普拉西肟和肟HI-6对塔苯中毒大鼠神经保护和再激活作用的比较
目的:比较肟K870联合阿托品对塔布恩中毒大鼠的神经保护和中枢再激活作用与标准解毒治疗的疗效。方法:在给药后2 h和24 h,采用功能观察电池法观察解毒剂治疗对亚致死剂量他苯中毒大鼠的神经保护作用,采用组织病理学法观察他苯所致脑损伤,采用标准分光光度法测定脑内乙酰胆碱酯酶活性,评价肟类药物的中枢再激活作用。结果:新研制的肟类药物K870的中枢再激活作用与普拉度肟的中枢再激活作用大致相当,而肟类药物HI-6的脑乙酰胆碱酯酶的再激活作用可以忽略不计。肟K870对tabun诱导的急性神经毒性的抑制作用略高于普拉度肟,与肟HI-6相似。这些结果大致符合tabun诱导的脑损伤的组织病理学评价。结论:新合成的肟类药物K870与目前研究的肟类药物相比,其神经保护作用仅略高或相近,不适合替代常用肟类药物用于急性塔苯中毒的解毒治疗。
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来源期刊
Acta medica (Hradec Kralove)
Acta medica (Hradec Kralove) Medicine-Medicine (all)
CiteScore
1.10
自引率
0.00%
发文量
8
审稿时长
20 weeks
期刊介绍: Acta Medica (Hradec Králové) is a multidisciplinary medical journal published by the Faculty of Medicine in Hradec Králové - Karolinum Press, the publishing house of Charles University. The journal is peer-reviewed and published quarterly in both paper and electronic form. The language of Acta Medica is English. Offerings include review articles, original articles, brief communications, case reports, announcements and notices. The journal was founded in 1958 under the title "A Collection of Scientific Works of the Charles University Faculty of Medicine in Hradec Kralove."
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