Hydroxylated analogs of mexiletine as tools for structural-requirements investigation of the sodium channel blocking activity

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Abstract

[2-(2-Aminopropoxy)-1,3-phenylene]dimethanol 1 and 4-(2-aminopropoxy)-3- (hydroxymethyl)-5-methylphenol 2, two dihydroxylated analogs of mexiletine - a well known class IB anti-arrhythmic drug - were synthesized and used as pharmacological tools to investigate the blockingactivity requirements of human skeletal muscle, voltage-gated sodium channel. The very low blocking activity shown by newly synthesized compounds corroborates the hypothesis that the presence of a phenolic group in the para-position to the aromatic moiety and/or benzylic hydroxyl groups on the aromatic moiety of local anesthetic-like drugs impairs either the transport to or the interaction with the binding site in the pore of Na+ channels. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.

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Catalano, A., Carocci, A., Cavalluzzi, M. M., Di Mola, A., Lentini, G., Lovece, A., … Franchini, C. (2010). Hydroxylated analogs of mexiletine as tools for structural-requirements investigation of the sodium channel blocking activity. Archiv Der Pharmazie, 343(6), 325–332. https://doi.org/10.1002/ardp.200900218

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