Title
Optimized Synthesis and Pharmacological Evaluation of HCN Channel Inhibitor EC18
Author
Patberg, Marius, 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, and Anna Junker
Year
2023
Journal
Archiv Der Pharmazie
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.
Instrument
unknown
Keywords
HCN channel,ion channels