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烷氧基苯基氨基甲酸酯类似物的镇咳活性

Antitussive activity of alcoxyphenyl carbamic acid analogues.

作者信息

Jurecekova Jana, Nosalova Gabriela, Jurecek Ludovit, Csollei Jozef, Sivova Veronika, Nosal Slavomir

机构信息

Biomedical Center Martin, Jessenius Faculty of Medicine, Comenius University in Bratislava, Malá Hora 4D, Martin, Slovakia.

出版信息

Gen Physiol Biophys. 2018 May;37(3):337-343. doi: 10.4149/gpb_2017048.

Abstract

In this study we report pharmacological evaluation of four newly synthetized analogues of alcoxyphenyl carbamic acid, structurally related to butamirate citrate that is frequently used as cough suppressing drug, and marked as ATK 231, ATK 241, ATK 251 and ATK 261. These agents with various modifications of the molecular structure have been tested for antitussive activity in cough induced by inhalation of aerosol of citric acid (0.3 M) over 3 minutes using conscious guinea pigs. Results revealed significant cough suppressing activity without significant influence on specific airways resistances in all tested substances. ATK 231 and ATK241 showed significantly higher total antitussive activities when compared to both codeine phosphate and butamirate citrate, while ATK 251 only comparing to butamirate citrate. We did not observe any notable adverse effects and these compounds could thus potentially represent promising new non-narcotic antitussives suitable for further studies.

摘要

在本研究中,我们报告了四种新合成的烷氧基苯基氨基甲酸酯类似物的药理学评估,它们在结构上与常用作止咳药物的枸橼酸布他米酯相关,分别标记为ATK 231、ATK 241、ATK 251和ATK 261。使用清醒的豚鼠,对这些具有不同分子结构修饰的药物进行了测试,以评估其在吸入3分钟0.3M柠檬酸气雾剂诱发咳嗽中的镇咳活性。结果显示,所有测试物质均具有显著的镇咳活性,且对特定气道阻力无显著影响。与磷酸可待因和枸橼酸布他米酯相比,ATK 231和ATK 241表现出显著更高的总镇咳活性,而ATK 251仅与枸橼酸布他米酯相比有此效果。我们未观察到任何明显的不良反应,因此这些化合物可能代表有前景的新型非麻醉性止咳药,适合进一步研究。

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