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Short- and long-term inhibition of cardiac inward-rectifier potassium channel current by an antiarrhythmic drug bepridil.
Ma, Fangfang; Takanari, Hiroki; Masuda, Kimiko; Morishima, Masaki; Ono, Katsushige.
Afiliação
  • Ma F; Department of Pathophysiology, Oita University School of Medicine, Yufu, 879-5593, Oita, Japan.
  • Takanari H; Department of Cardiology, The 1st Hospital of Hebei Medical University, Shijiazhung, 050031, Hebei, China.
  • Masuda K; Department of Pathophysiology, Oita University School of Medicine, Yufu, 879-5593, Oita, Japan.
  • Morishima M; Department of Pathophysiology, Oita University School of Medicine, Yufu, 879-5593, Oita, Japan.
  • Ono K; Department of Pathophysiology, Oita University School of Medicine, Yufu, 879-5593, Oita, Japan.
Heart Vessels ; 31(7): 1176-84, 2016 Jul.
Article em En | MEDLINE | ID: mdl-26498939
Bepridil is an effective antiarrhythmic drug on supraventricular and ventricular arrhythmias, and inhibitor of calmodulin. Recent investigations have been elucidating that bepridil exerts antiarrhythmic effects through its acute and chronic application for patients. The aim of this study was to identify the efficacy and the potential mechanism of bepridil on the inward-rectifier potassium channel in neonatal rat cardiomyocytes in acute- and long-term conditions. Bepridil inhibited inward-rectifier potassium current (I K1) as a short-term effect with IC50 of 17 µM. Bepridil also reduced I K1 of neonatal cardiomyocytes when applied for 24 h in the culture medium with IC50 of 2.7 µM. Both a calmodulin inhibitor (W-7) and an inhibitor of calmodulin-kinase II (KN93) reduced I K1 when applied for 24 h as a long-term effect in the same fashion, suggesting that the long-term application of bepridil inhibits I K1 more potently than that of the short-term application through the inhibition of calmodulin kinase II pathway in cardiomyocytes.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Bepridil / Canais de Potássio Corretores do Fluxo de Internalização / Bloqueadores dos Canais de Potássio / Miócitos Cardíacos / Antiarrítmicos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Ano de publicação: 2016 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Bepridil / Canais de Potássio Corretores do Fluxo de Internalização / Bloqueadores dos Canais de Potássio / Miócitos Cardíacos / Antiarrítmicos Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Ano de publicação: 2016 Tipo de documento: Article