Ex Vivo and In Vivo Study of Some Isoquinoline Precursors

IF 2.3 Q3 PHARMACOLOGY & PHARMACY Scientia Pharmaceutica Pub Date : 2022-06-13 DOI:10.3390/scipharm90020037

M. Milusheva, V. Gledacheva, Margarita Batmazyan, S. Nikolova, I. Stefanova, D. Dimitrova, K. Saracheva, D. Tomov, Veneta Chaova-Gizdakova

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引用次数: 5

Abstract

This article concerns the synthesis and biological activities of some N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides as isoquinoline precursors and compounds with smooth muscle (SM) relaxant activity. Aim: find the biological activity of N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides and compare it with papaverine, an isoquinoline alkaloid that has been known as a brain and coronary vasodilator and SM relaxant. Materials and methods: In silico simulation with the PASS online program predicts SM relaxant activity for the compounds. The amides were tested on the isolated gastric SM preparations (SMPs) from rats to determine their effects on spontaneous contractile activity (CA) compared with papaverine. The in vivo effect on the learning and memory processes of rats was also assessed. Results: the data from the isometric measurements showed that one of the compounds caused ex vivo relaxation in circular SM tissues isolated from the stomach (corpus) of male Wistar rats. Conclusion: We found that the compound’s SM relaxation uses the papaverine pathway. It also has an improving effect on the cognitive functions of learning and memory processes in rats.

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某些异喹啉前体的离体和体内研究

本文研究了异喹啉前体N-(1-(3,4-二甲氧基苯基)丙烯-2-基)酰胺类化合物的合成及其生物活性。目的:发现N-(1-(3,4-二甲氧基苯基)丙基-2-基)酰胺的生物活性，并将其与罂粟碱进行比较，罂粟碱是一种异喹啉生物碱，被称为脑和冠状动脉舒张剂和SM松弛剂。材料和方法:利用PASS在线程序进行硅模拟，预测化合物的SM松弛活性。用离体大鼠胃SM制剂(SMPs)测定其与罂粟碱比较对自发性收缩活性(CA)的影响。并评估其在体内对大鼠学习记忆过程的影响。结果:等长测量数据显示，其中一种化合物引起雄性Wistar大鼠胃(体)圆形SM组织的体外松弛。结论:该化合物的SM松弛作用是通过罂粟碱途径实现的。对大鼠学习记忆过程的认知功能也有改善作用。

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