Suppr超能文献

[寻找前庭保护剂的新方法]

[A new approach to the search for vestibuloprotectors].

作者信息

Yasnetsov V V, Karsanova S K, Yasnetsov Vic V

出版信息

Aviakosm Ekolog Med. 2015;49(1):5-12.

Abstract

The results of experimental clinical testing of the antinaupathia action of as new compounds, so motion sickness medications (promethazine, ikaron-1 etc.) are presented. Russian medication mexidol, a derivative of 3-hydroxypyridine (3-HP) demonstrated the ability to control motion sickness in humans and animals; however, unlike reference vestibuloprotector scopolamine, it does not practically produce side-effects. Mexidol acts through ion pathways with the involvement of glutamate and GABA-ergic components. Revealed 9 of new 3-HP derivates with an antimotion sickness effect in rats, three exceeded in efficacy mexidol, and also reference medications (i.e. scopolamine and promethazine). Melatonin achieves a better vestiboloprotective effect in rats than promethazine and melatonin-ergic antidepressant agomelatine through the involvement of melatonin MT1-, MT2- and GABA(A)-receptors. Also, combinations of melatonin with mexidol or promethazine possess a distinct vestibuloprotective effect, as melatonin enhances the action of equally mexidol and promethazine. Analysis of our results and investigations of other authors infer that search for potent vestibuloprotectors should be extended to new 3-HP derivatives and melatoninergic compounds. Individual medications by themselves and in combinations can become a solution to the problem.

摘要

本文展示了作为新型化合物的抗晕动病药物(如异丙嗪、伊卡隆 -1 等)的实验临床测试结果。俄罗斯药物美西多福,一种 3 - 羟基吡啶(3 - HP)的衍生物,已证明其在人和动物中具有控制晕动病的能力;然而,与参比前庭保护剂东莨菪碱不同,它几乎不会产生副作用。美西多福通过离子途径发挥作用,涉及谷氨酸和 GABA 能成分。在大鼠中发现了 9 种具有抗晕动病作用的新型 3 - HP 衍生物,其中三种在功效上超过了美西多福,也超过了参比药物(即东莨菪碱和异丙嗪)。褪黑素通过涉及褪黑素 MT1、MT2 和 GABA(A) 受体,在大鼠中比异丙嗪和褪黑素能抗抑郁药阿戈美拉汀具有更好的前庭保护作用。此外,褪黑素与美西多福或异丙嗪的组合具有明显的前庭保护作用,因为褪黑素增强了美西多福和异丙嗪的作用。对我们的结果以及其他作者研究的分析表明,寻找有效的前庭保护剂应扩展到新型 3 - HP 衍生物和褪黑素能化合物。单独使用或联合使用的个别药物可能成为解决该问题的方法。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验