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.
Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18 / Patberg, Marius; Oniani, Tengiz; Disse, Paul; Peischard, Stefan; Vinnenberg, Laura; Zobeiri, Mehrnoush; Romanelli, Maria N; Epping, Lisa; Wiendl, Heinz; Meuth, Sven G; Hundehege, Petra; Seebohm, Guiscard; Budde, Thomas; Junker, Anna. - In: ARCHIV DER PHARMAZIE. - ISSN 0365-6233. - ELETTRONICO. - (2023), pp. e2200665.0-e2200665.0. [10.1002/ardp.202200665]
Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18
Romanelli, Maria N;
2023
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.
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Archiv der Pharmazie - 2023 - Patberg - Optimized synthesis and pharmacological evaluation of HCN channel inhibitor EC18 (1).pdf
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