Inhibition of skeletal muscle sodium currents by mexiletine analogues: specific hydrophobic interactions rather than lipophilia per se account for drug therapeutic profile


In striated fibers, the activity of mexiletine (Mex)-like sodium channel blockers is strongly modulated by the part of the molecule nearby the asymmetric carbon atom. A lipophilic aromatic phenyl group at this levels, as in 2-(2,6-dimethylphenoxy)-1-phenylethanamine (Me4), markedly increases drug potency, while an increased distance between the stereogenic… (More)
DOI: 10.1007/s00210-002-0669-0


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