tcsc3590 Lappaconitine (hydrobromide)

Lappaconitine hydrobromide, a diterpene alkaloid, is a drug for the treatment of cardiac arrhythmias.

IC50 value:

Target: A natural product for anti-cardiac arrhythmias

In vitro: Lappaconitine hydrobromide was found to exert an inhibitory effect on inward tetrodotoxin-sensitive sodium currents without changing their voltage dependence [1].

In vivo: The effect of Lappaconitine hydrobromide on aconitine--induced arrhythmias is due to modulation of genes encoding Na(+)-, K(+)-, Ca(2+)-channels, conducting ionic currents (I(Na), I(to), I(Ks), I(K1), I(CaT)), which are involved in the formation of different phases of the action potential [2]. Lappaconitine hydrobromide was found to be beneficial both in ventricular and supraventricular premature beats. Oral allapinine usually showed its effect 40-60 minutes following its administration, its maximum action being 4-5 hours later, its duration was some 8 hours. The optimal dose of the drug amounted to 75 mg/day [3].