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. 2009 Apr;44(4):1477-85.
doi: 10.1016/j.ejmech.2008.10.005. Epub 2008 Oct 14.

2D- and 3D-QSAR of tocainide and mexiletine analogues acting as Na(v)1.4 channel blockers

Antonio Carrieri  1 , Marilena Muraglia, Filomena Corbo, Concetta Pacifico
Affiliations

2D- and 3D-QSAR of tocainide and mexiletine analogues acting as Na(v)1.4 channel blockers

Antonio Carrieri et al. Eur J Med Chem. 2009 Apr.

Abstract

Enantiomeric forms of Tocainide, Mexiletine, and structurally related local anaesthetic compounds, were analyzed with respect to their potency in blocking Na(v)1.4 channel. Structure-activity relationships based on in vitro pharmacological assays, suggested that an increase in terms of lipophilicity and/or molecular surface as well as the presence of specific polar spacers might be determinant for receptor interactions. QSAR and pharmacophore models were then used to support at 3D level this hypothesis.

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