SELECTIVE CLASS-III ANTIARRHYTHMIC AGENTS .1. BIS(ARYLALKYL)AMINES
SELECTIVE CLASS-III ANTIARRHYTHMIC AGENTS .1. BIS(ARYLALKYL)AMINES
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DOI：
10.1021/jm00166a011
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发表时间：
1990-04-01
影响因子：
7.3
通讯作者：
HIGGINS, AJ
中科院分区：
文献类型：
--
作者：
CROSS, PE;ARROWSMITH, JE;HIGGINS, AJ
本文介绍了一系列双芳烷基胺类化合物，并列举了它们延长离体心脏组织有效不应期的作用。大多数化合物延长心脏动作电位，而不显着改变最大速率的去极化，可被定义为选择性III类抗心律失常药物。发现特别有利的结构特征是在两个芳环上具有甲磺酰氨基部分。因此，选择化合物16 [1-（4-甲磺酰氨基苯氧基）-2-[N-（4-甲磺酰氨基苯乙基）-N-甲胺]乙烷]用于进一步研究。该化合物是高效且选择性的III类药物，通过阻断心脏钾通道发挥作用。
A series of bis(arylalkyl)amines is described and their effects on prolonging effective refractory period in isolated cardiac tissue listed. Most compounds prolonged the cardiac action potential without significantly altering the maximum rate of depolarization and may be defined as selective class III antiarrhythmic agents. It was found that a particularly advantageous structural feature was to have a methanesulfonamido moiety on both of the aryl rings. Thus, compound 16 [1-(4-methanesulfonamidophenoxy)-2-[N-(4-methanesulfonamidophenethyl)-N-methylamine]ethane] was selected for further investigations. The compound is highly potent and selective class III agent which acts by blockade of cardiac potassium channels.