Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18

HCN通道抑制剂EC18的优化合成及药理评价

阅读:7
作者:Marius Patberg, Tengiz Oniani, Paul Disse, Stefan Peischard, Laura Vinnenberg, Mehrnoush Zobeiri, Maria N Romanelli, Lisa Epping, Heinz Wiendl, Sven G Meuth, Petra Hundehege, Guiscard Seebohm, Thomas Budde, Anna Junker

Abstract

HCN4 channels are considered to be a promising target for cardiac pathologies, epilepsy, and multiple sclerosis. However, there are no subtype-selective HCN channel blockers available, and only a few compounds are reported to display subtype preferences, one of which is EC18 (cis-1). Herein, we report the optimized synthetic route for the preparation of EC18 and its evaluation in three different pharmacological models, allowing us to assess its activity on cardiac function, thalamocortical neurons, and immune cells.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。