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Common Molecular Determinants of Flecainide and Lidocaine Block of Heart Na(+) Channels: Evidence from Experiments with Neutral and Quaternary Flecainide Analogues

Flecainide (pKa 9.3, 99% charged at pH 7.4) and lidocaine (pKa 7.6–8.0, ∼50% neutral at pH 7.4) have similar structures but markedly different effects on Na(+) channel activity. Both drugs cause well-characterized use-dependent block (UDB) of Na(+) channels due to stabilization of the inactivated st...

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Detalles Bibliográficos
Autores principales: Liu, Huajun, Atkins, Joshua, Kass, Robert S.
Formato: Texto
Lenguaje:English
Publicado: The Rockefeller University Press 2003
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2217334/
https://www.ncbi.nlm.nih.gov/pubmed/12601084
http://dx.doi.org/10.1085/jgp.20028723