含有天然单萜结构的心得安类似物:合成和药理学性质。

A Siemieniuk, H Szałkowska-Pagowska, S Lochyński, K Piatkowski, B Filipek, J Krupińska, R Czarnecki, T Librowski, S Białas
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引用次数: 0

摘要

合成了几种天然双环单萜衍生物,它们是心得安的类似物。对这些化合物进行药理学研究,以确定其毒性,在心律失常实验模型中的抗心律失常活性,局部麻醉作用和对心血管系统的影响。在钡性心律失常模型中,所测试的化合物对参比药物的毒性较小或相似,缺乏抗心律失常活性,但其中一些化合物(化合物9和12)增加了strophanthin的致心律失常剂量。所研究的所有化合物在浸润麻醉中都比利多卡因有更强的局部麻醉作用,化合物8在表面麻醉中也比利多卡因强。
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Propranolol analogs containing natural monoterpene structures: synthesis and pharmacological properties.

A few derivatives of natural, bicyclic monoterpenes, which are propranolol analogs, were synthetized. Those compounds were studied pharmacologically in order to determine their toxicity, antiarrhythmic activity in selected experimental models of arrhythmia, the local anesthetic effect and influence on the cardiovascular system. The tested compounds showed a less potent or similar toxicity towards reference drugs, were devoid of an antiarrhythmic activity in the model of barium arrhythmia, yet some of them (compounds 9 and 12) increased the arrhythmogenic dose of strophanthin. All the compounds studied had a local anesthetic effect stronger than lidocaine in infiltration anesthesia, and compound 8--also in surface anesthesia.

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