Selective Kv1.5 Blockers: Development of (R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a Potential Treatment for Atrial

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• 作者：Benjamin E. Blass ; Andrew Fensome ; Eugene Trybulski ; Ronald Magolda ; Stephen J. Gardell ; Kun Liu ; Manoj Samuel ; Irene Feingold ; Christine Huselton ; Chris M. Jackson ; Laurent Djandjighian ; Douglas Ho
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：November 12, 2009
• 年：2009
• 卷：52
• 期：21
• 页码：6531-6534
• 全文大小：743K
• 年卷期：v.52,no.21(November 12, 2009)
• ISSN：1520-4804

文摘

Atrial fibrillation is the most prevalent form of cardiac arrhythmia. Current treatments extend the atrial effective refractory period by nonselective blockade of cardiac ion channels. An alternative approach selectively targeting the Kv1.5 ion channel offers the opportunity for therapeutic benefit with decreased risk of adverse cardiovascular events. KVI-020 (4g) successfully demonstrated antiarrhythmic efficacy in a canine arrhythmia model, and these findings support its utility as an antiarrhythmic agent.