某些含金属硫酸化合物的抗惊厥作用

Shukurov Shukurov, B. E.V., Shukurov Al. S., Zalogin S.D., S. E.V.
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引用次数: 0

摘要

研究了2-氨基乙烷磺酸镁-双乙酰氨基-2-氨基乙烷磺酸盐(LHT-317)和锌-环-双乙酰氨基-2-氨基乙烷磺酸盐(LHT-318)衍生物的抗惊厥活性。实验用30只实验用白色大鼠,通过腹腔注射320mg /kg盐酸匹罗卡品建立癫痫模型。在癫痫形成后的4周内,以该给药方式给药大鼠LD50的2.5%和5%分别给药LHT-31、LHT-318和卡马西平。以卡马西平为对照药。采用克鲁辛斯基量表评估发作频率、持续时间和严重程度。脑海马和齿状沟的形态学研究采用0.4%甲酚紫尼氏染色。使用奥林巴斯Bx50数码显微镜对结果进行评估,放大倍数为x400,面积为1000µm2。2-氨基乙磺酸LHT-318锌盐表现出抗惊厥特性:降低急性惊厥发作的严重程度,阻止自发惊厥活动的形成,其活性与参比药物卡马西平相当。LHT-317在该模型中未显示出抗癫痫活性。化合物LHT-317和LHT-318在给药过程中阻止了匹罗卡品癫痫发生特征的形态改变深度,但应该强调的是,在任何情况下都没有观察到完全预防形态障碍。因此,基于本研究,我们可以认为2-氨基乙磺酸锌环盐可以作为治疗癫痫的潜在药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
ANTI-CONVULSIVE EFFECTS OF SOME METAL-CONTAINING SULFIC ACID COMPOUNDS
The anticonvulsant activity of 2-aminoethanesulfonic derivatives - magnesium bis-acetamino-2-aminoethanesulfonate (LHT-317) and zinc cyclo-bis-acetamino-2-aminoethanesulphonate (LHT-318) derivatives was studied in the model of pilacorpine epileptogenesis. The studies were performed on 30 white laboratory rats, in which epilepsy was modeled by intraperitoneal administration of pilocarpine hydrochloride at a dose of 320 mg/kg. Within 4 weeks after the formation of epilepsy rats were got intragastrically LHT-31, LHT-318 and Carbamazepine at doses of 2.5% and 5% of the LD50 determined for rats with this route of administration. Carbamazepine was used as the reference drug. The frequency, duration and severity of seizures were assessed using the Krushinsky scale. Morphological studies of the brain in the hippocampus and dentate sulcus were profiled by Nissl staining using 0.4% cresyl violet. The results were evaluated using an Olympus Bx50 digital microscope, x400 magnification over an area of 1000 µm2. The zinc salt of 2-aminoethanesulfonic acid LHT-318 exhibited anticonvulsant properties: it reduced the severity of acute convulsive paroxysm, prevented the formation of spontaneous convulsive activity, and was comparable in activity to the reference drug carbamazepine. LHT-317 did not demonstrate antiepileptic activity in this model. Compounds LHT-317 and LHT-318 at course administration prevented the depth of morphological changes characteristic of pilocarpine epileptogenesis, while it should be emphasized that complete prevention of morphological disorders is not observed in any case. Thus, based on the study, we can conclude that the zinc cyclic salt of 2-aminoethanesulfonic acid can be considered as a potential drug for the treatment of epilepsy.
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