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Modulation of the transient outward current (Ito) in rat cardiac myocytes and human Kv4.3 channels by mefloquine.
Perez-Cortes, E J; Islas, A A; Arevalo, J P; Mancilla, C; Monjaraz, E; Salinas-Stefanon, E M.
Afiliação
  • Perez-Cortes EJ; Laboratory of Cardiac Biophysics, Instituto de Fisiología and Facultad de Medicina, Universidad Autónoma de Puebla, Puebla, Mexico.
  • Islas AA; Laboratory of Cardiac Biophysics, Instituto de Fisiología and Facultad de Medicina, Universidad Autónoma de Puebla, Puebla, Mexico.
  • Arevalo JP; Laboratory of Cardiac Biophysics, Instituto de Fisiología and Facultad de Medicina, Universidad Autónoma de Puebla, Puebla, Mexico.
  • Mancilla C; Laboratory of Cardiac Biophysics, Instituto de Fisiología and Facultad de Medicina, Universidad Autónoma de Puebla, Puebla, Mexico.
  • Monjaraz E; Laboratory of Cardiac Biophysics, Instituto de Fisiología and Facultad de Medicina, Universidad Autónoma de Puebla, Puebla, Mexico.
  • Salinas-Stefanon EM; Laboratory of Cardiac Biophysics, Instituto de Fisiología and Facultad de Medicina, Universidad Autónoma de Puebla, Puebla, Mexico. Electronic address: eduardo.salinas@correo.buap.mx.
Toxicol Appl Pharmacol ; 288(2): 203-12, 2015 Oct 15.
Article em En | MEDLINE | ID: mdl-26216464
The antimalarial drug mefloquine, is known to be a potassium channel blocker, although its mechanism of action has not being elucidated and its effects on the transient outward current (Ito) and the molecular correlate, the Kv4.3 channel has not being studied. Here, we describe the mefloquine-induced inhibition of the rat ventricular Ito and of CHO cells co-transfected with human Kv4.3 and its accessory subunit hKChIP2C by whole-cell voltage-clamp. Mefloquine inhibited rat Ito and hKv4.3+KChIP2C currents in a concentration-dependent manner with a limited voltage dependence and similar potencies (IC50=8.9µM and 10.5µM for cardiac myocytes and Kv4.3 channels, respectively). In addition, mefloquine did not affect the activation of either current but significantly modified the hKv4.3 steady-state inactivation and recovery from inactivation. The effects of this drug was compared with that of 4-aminopyridine (4-AP), a well-known potassium channel blocker and its binding site does not seem to overlap with that of 4-AP.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Potenciais de Ação / Ativação do Canal Iônico / Mefloquina / Bloqueadores dos Canais de Potássio / Miócitos Cardíacos / Canais de Potássio Shal / Antimaláricos Limite: Animals Idioma: En Revista: Toxicol Appl Pharmacol Ano de publicação: 2015 Tipo de documento: Article País de afiliação: México País de publicação: Estados Unidos
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Potenciais de Ação / Ativação do Canal Iônico / Mefloquina / Bloqueadores dos Canais de Potássio / Miócitos Cardíacos / Canais de Potássio Shal / Antimaláricos Limite: Animals Idioma: En Revista: Toxicol Appl Pharmacol Ano de publicação: 2015 Tipo de documento: Article País de afiliação: México País de publicação: Estados Unidos