New potent mexiletine and tocainide analogues evaluated in vivo and in vitro as antimyotonic agents on the myotonic ADR mouse
A De Luca, S Pierno, A Liantonio, JF Desaphy… - Neuromuscular …, 2004 - Elsevier
The antimyotonic activity of chiral derivatives of mexiletine and tocainide, selected as potent
use-dependent blockers of skeletal muscle sodium channels, was evaluated in vivo acutely
in myotonic ADR mice. The compounds had either aromatic (Me4 and Me6) or branched
isopropyl groups (Me5 and To1) on the asymmetric centre, or had this latter one methylene
apart from the amino group (Me2). Therapeutic doses of mexiletine (5–10 mg/kg) and
tocainide (7–20 mg/kg) significantly reduced the long time of righting reflex (TRR), typical of …
use-dependent blockers of skeletal muscle sodium channels, was evaluated in vivo acutely
in myotonic ADR mice. The compounds had either aromatic (Me4 and Me6) or branched
isopropyl groups (Me5 and To1) on the asymmetric centre, or had this latter one methylene
apart from the amino group (Me2). Therapeutic doses of mexiletine (5–10 mg/kg) and
tocainide (7–20 mg/kg) significantly reduced the long time of righting reflex (TRR), typical of …