It is a selective blocker of the TTX-sensitive Na⁺ channel in the heart, a potent antiarrhythmic belonging to the Id class, an antifibrillatory, an anti-inflammatory and a local anesthetic agent. It presents micromolar affinity at brain Alpha-Bungarotoxin-sensitive nAChR.

N-Deacetyllappaconitine possesses a potent anti-arrhythmic and antifibrillatory action in various forms of extrasystolic and systolic arrhythmias. 0.5-1 mg/kg (i.v.) prevent and stop arrhythmias induced by Aconitine, Ba chloride, electric stimulation and occlusion of the coronary artery. Comparatively to many antiarrhythmic drugs, at the dosage producing a strong antiarrhytmic effect, it does not lower the systemic arterial pressure, does not possess negative and inotropic or chronotropic action and slightly acts upon the refractory period and the Q-T interval.

N-Deacetyllappaconitine interacts selectively with TTX-sensitive Na⁺ channel and suppresses the Na⁺ current without changing the channel activation threshold, which has been established using patch clamp and intracellular perfusion on isolated cardiomyocytes and neurons from rat ganglia.
It has also been established that N-Deacetyllappaconitine acts as a local anaesthetic and as an anti-inflammatory.

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For research use only — not intended for food, diagnostic or therapeutic use