Literature DB >> 19888755

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 arrhythmia.

Benjamin E Blass1, Andrew Fensome, Eugene Trybulski, Ronald Magolda, Stephen J Gardell, Kun Liu, Manoj Samuel, Irene Feingold, Christine Huselton, Chris M Jackson, Laurent Djandjighian, Douglas Ho, James Hennan, John M Janusz.   

Abstract

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.

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Year:  2009        PMID: 19888755     DOI: 10.1021/jm901042m

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  2 in total

1.  Rotor termination is critically dependent on kinetic properties of I kur inhibitors in an in silico model of chronic atrial fibrillation.

Authors:  Eberhard P Scholz; Paola Carrillo-Bustamante; Fathima Fischer; Mathias Wilhelms; Edgar Zitron; Olaf Dössel; Hugo A Katus; Gunnar Seemann
Journal:  PLoS One       Date:  2013-12-20       Impact factor: 3.240

Review 2.  Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5.

Authors:  Zefeng Zhao; Songsong Ruan; Xiaoming Ma; Qian Feng; Zhuosong Xie; Zhuang Nie; Peinan Fan; Mingcheng Qian; Xirui He; Shaoping Wu; Yongmin Zhang; Xiaohui Zheng
Journal:  Biomolecules       Date:  2019-12-19
  2 in total

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