1237512-75-2Relevant academic research and scientific papers
Hydroxylated analogs of mexiletine as tools for structural-requirements investigation of the sodium channel blocking activity
Catalano, Alessia,Carocci, Alessia,Cavalluzzi, Maria M.,Di Mola, Antonia,Lentini, Giovanni,Lovece, Angelo,Dipalma, Antonella,Costanza, Teresa,Desaphy, Jean-Francois,Camerino, Diana Conte,Franchini, Carlo
, p. 325 - 332 (2011/07/29)
[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.
