Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18

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

Research article (journal) | Peer reviewed

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.

Details about the publication

JournalArchiv der Pharmazie / Chemistry in Life Sciences (ArchPharm)
Volumee2200665
StatusPublished
Release year2023
Language in which the publication is writtenEnglish
DOI10.1002/ardp.202200665
Link to the full texthttps://api.elsevier.com/content/abstract/scopus_id/85150907138
KeywordsEC18; iPSC; ion channels; HCN4; HCN channel

Authors from the University of Münster

Budde, Thomas
Institute of Physiology I (Neurophysiology)
Hundehege, Petra
Department for Neurology
Seebohm, Guiscard
Institut für Genetik von Herzerkrankungen (IfGH)
Zobeiri, Mehrnoush
Institute of Physiology I (Neurophysiology)