May H J, Kretzschmar R, Neumann W, Gries J
Arzneimittelforschung. 1980;30(9):1487-93.
Several 1-, 3-, and 6-substituted 3-amino-1H-isoindoles have been synthesized and screened for biological properties. In pharmacological testing significant and long-lasting local-anesthetic activity was found even in low concentrations. Subsequently, investigations for antiarrhythmic properties were carried out. The same or even higher activity compared to quinidine sulfate was found on isolated guinea pig atria (refractory period prolongation), anaesthetized rats (aconitine induced arrhythmias), guinea pigs (electrically induced cardiac fibrillation) and in conscious dogs with arrhythmias due to coronary artery occlusion. Unfortunately, antiarrhythmic doses caused toxic symptoms in dogs.
已合成了几种1-、3-和6-取代的3-氨基-1H-异吲哚，并对其进行了生物学特性筛选。在药理测试中，即使在低浓度下也发现了显著且持久的局部麻醉活性。随后，开展了抗心律失常特性的研究。在离体豚鼠心房（延长不应期）、麻醉大鼠（乌头碱诱发心律失常）、豚鼠（电诱发心脏纤颤）以及因冠状动脉阻塞而出现心律失常的清醒犬中，发现了与硫酸奎尼丁相当甚至更高的活性。遗憾的是，抗心律失常剂量在犬身上引发了毒性症状。
