European Institute for Molecular Imaging (EIMI), Münster, Germany.
Institut für Physiologie I, Münster, Germany.
Arch Pharm (Weinheim). 2023 Jun;356(6):e2200665. doi: 10.1002/ardp.202200665. Epub 2023 Mar 22.
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.
HCN4 通道被认为是心脏病理学、癫痫和多发性硬化症的有前途的治疗靶点。然而，目前还没有亚型选择性的 HCN 通道阻滞剂，只有少数几种化合物被报道具有亚型偏好性，其中一种是 EC18（顺式-1）。本文报道了 EC18 的优化合成路线，并在三种不同的药理学模型中对其进行了评估，从而可以评估其对心脏功能、丘脑皮质神经元和免疫细胞的活性。
