Possibility of pharmacological correction of NMDA-induced retinal excitotoxicity by 3-hydroxypyridine derivatives

N. V. Solovev
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Abstract

Relevance. Glaucoma is the leading cause of blindness worldwide. Among all pathological mechanisms, a special role is assigned to glutamate excitotoxicity, which accompanies a number of pathological conditions of the retina. The aim of this work was to study the pharmacological activity of compounds of 3-hydroxypyridine derivatives in a model of NMDA-induced retinal degeneration. Material and methods. The introduction of the compounds was carried out in the prophylactic mode of administration. 7 days after the model, ophthalmoscopic changes in the fundus and the level of microcirculation were assessed. Research results. According to the results of the study, it was found that the compound LHT 6-20 had the highest activity. Compound LHT 6-20 at a dose of 25.5 mg/ kg in a model of neurodegenerative retinal damage induced by intravitreal administration of NMDA in rats with a prophylactic administration regimen provides an improvement in the fundus picture by 15.4%, relative to the group with a pathology model, which has a statistically a significant difference (p < 0.05), an increase in the level of microcirculation in the retina by 14.1% relative to the group with the model, while the indicator has a statistically significant difference from the group with pathology (p < 0.05), but does not differ from the reference drug (p > 0.05). Keywords: derivatives of 3-hydroxypyridine, NMDA, excitotoxicity, retina, rats, the level of microcirculation, ophthalmoscopy
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3-羟基吡啶衍生物对nmda诱导的视网膜兴奋性毒性的药理学纠正可能性
的相关性。青光眼是全世界致盲的主要原因。在所有的病理机制中,谷氨酸兴奋性毒性被赋予了一个特殊的作用,它伴随着视网膜的一些病理条件。本研究的目的是研究3-羟基吡啶衍生物化合物在nmda诱导的视网膜变性模型中的药理活性。材料和方法。化合物的引入是以预防性给药的方式进行的。造模7 d后,观察眼底变化及微循环水平。研究的结果。根据研究结果,发现化合物LHT 6-20的活性最高。复合LHT 6 20剂量为25.5毫克/公斤在模型中诱导的神经退行性视网膜损害intravitreal管理NMDA对老鼠的预防性管理方案提供了一个改善眼底照片15.4%,相对于与病理模型组,有统计学显著性差异(p < 0.05),增加视网膜微循环水平14.1%相对于组模型,而该指标与病理组比较差异有统计学意义(p < 0.05),与对照药物比较差异无统计学意义(p > 0.05)。关键词:3-羟基吡啶衍生物,NMDA,兴奋毒性,视网膜,大鼠,微循环水平,检眼镜
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