新型 3-氰基-1,4-二氢吡啶、氰基乙酰胺衍生物在急性福尔马林水肿模型上的抗渗出活性研究

A. V. Bochev, E. Bibik, S. Krivokolysko, K. Frolov
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摘要

大多数病症都伴随着炎症过程,需要药物治疗。尽管科学家们在医学和药理学领域取得了巨大成就,但现有的类固醇和非类固醇抗炎药物仍有许多不良反应。迄今为止,最紧迫的方向之一就是寻找有效、安全且具有抗炎活性的新药。本研究的目的是在经典的急性福尔马林水肿试验中研究新的 3-氰基-1,4-二氢吡啶、氰硫乙酰胺衍生物的抗渗出特性。材料和方法研究以 88 只体重 210-250 克的白鼠为对象。在急性福尔马林水肿模型中测定化合物的有效性。通过与参考药物布洛芬、吲哚美辛、美洛昔康和甲脒唑钠进行比较,对渗出的严重程度进行了计量评估。在诱发炎症前 1.5 小时,以 5 毫克/千克的剂量在胃内注射所研究的药物。研究结果研究发现,一些化合物具有抗渗出活性,其活性更明显或与参考药物的活性相似。代码为 mar-137 的实验室样本是领先样本,表现优于对比样本;在水肿模型建立 24 小时后,它的抗渗出效力超过布洛芬(2.39%)和甲咪唑钠(4.77%),抗炎效果与吲哚美辛和美洛昔康相似。结论实验室新合成的 3-氰基-1,4-二氢吡啶、氰基硫代乙酰胺衍生物样本具有明显的抗渗出活性,作为一类新型抗炎药物值得进一步研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Study of the anti-exudative activity of new 3-cyano-1,4- dihydropyridines, cyanotioacetamide derivatives, on the model of acute formalin edema
The inflammatory process accompanies most of the pathologies and requires pharmacological correction. In spite of significant achievements of scientists in the field of medicine and pharmacology, existing steroid and nonsteroidal antiinflammatory drugs have a number of undesirable reactions. To date, one of the most urgent directions is the search for new effective and safe drugs with anti-inflammatory activity. The aim of the study was to investigate the anti-exudative properties of new 3-cyano-1,4-dihydropyridines, cyanothioacetamide derivatives in the classical test of acute formalin edema. Material and methods. The study was conducted on 88 white rats weighing 210–250 g. The effectiveness of compounds was determined in a model of acute formalin edema, which was induced by subplantar injection of 0.1 ml of 2 % formalin solution into the right hind limb of the animals. The severity of exudation was evaluated oncometrically in comparison with reference drugs – ibuprofen, indomethacin, meloxicam and metamizole sodium. The studied substances were administered intragastrically at a dose of 5 mg/kg 1.5 hours before the induction of inflammation. Results. It was found that some compounds exhibit anti-exudative activity, more pronounced or similar to the activity of reference drugs. The laboratory sample with code mar-137 was the leading sample and outperformed the comparators; 24 hours after the modeling of edema, it exceeded ibuprofen (by 2.39 %), metamizole sodium (by 4.77 %) in anti-exudative efficacy and had an anti-inflammatory effect similar to the activity of indomethacin and meloxicam. Conclusions. Newly synthesized laboratory samples of 3-cyano-1,4-dihydropyridines, cyanothioacetamide derivatives, were found to exhibit pronounced anti-exudative activity and are of interest for further research as a new class of anti-inflammatory drugs.
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