phkineticaФармакокинетика и ФармакодинамикаPharmacokinetics and Pharmacodynamics2587-78362686-8830ООО «Издательство ОКИ»10.37489/2587-7836-2023-2-3-13phkinetica-366Research ArticleАКТУАЛЬНЫЕ ОБЗОРЫCURRENT REVIEWSКардиопротекторные средства с биароматической структурой. Часть 5. Блокаторы калиевых каналов Kv1.5Сardioprotective agents with biaromatic structure. Part 5. Potassium Kv1.5-channels blockershttps://orcid.org/0000-0003-2617-0334МокровГ. В.MokrovG. V.

к. х. н., в. н. с. лаборатории тонкого органического синтеза отдела химии лекарственных средств

Москва

Grigory V. Mokrov - PhD, Cand. Chemical Sci., Leading researcher of the fine organic synthesis laboratory at the drug chemistry department

Moscow

g.mokrov@gmail.comФГБНУ «Научно-исследовательский институт фармакологии имени В.В. Закусова»РоссияFSBI "Research Zakusov Institue of Pharmacology"Russian Federation20231807202302313Copyright © Мокров Г.В., 20232023Мокров Г.В.Mokrov G.V.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.pharmacokinetica.ru/jour/article/view/366

Калиевый канал Kv1.5 обеспечивает сверхбыстрый ток замедленного выпрямления IKur, который действует избирательно в клетках предсердий человека. Благодаря этому избирательная блокада Kv1.5 является перспективным подходом к контролю предсердных аритмий без неблагоприятных желудочковых эффектов, характерных для классических блокаторов калиевых каналов hERG-подтипа (Kv11.1). В натоящем обзоре рассмотрены все известные на сегодняшний день блокаторы Kv1.5-канала с биароматической структурой и данные об их биологических свойствах. Для многих исследованных Kv1.5-селективных соединений подтверждена способность препятствовать развитию предсердных аритмий без влияния на желудочковую рефрактерность.

The Kv1.5 potassium channel provides an ultra-rapid delayed rectifier potassium current, IKur, that acts selectively in human atrial cells. This makes selective Kv1.5 blockade a promising approach to control atrial arrhythmias without the adverse ventricular effects associated with classical hERG-subtype potassium channel blockers (Kv11.1). This review considers all currently known Kv1.5-channel blockers with a biaromatic structure and data on their biological properties. For many of the Kv1.5-selective compounds studied, the ability to prevent the development of atrial arrhythmias without affecting ventricular refractoriness was confirmed.

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The authors declare that there are no conflicts of interest present.