a selective blocker of the TTX-sensitive Na⁺ channel in the heart; potent antiarrhythmic belonging to the I_d class; antifibrillatory ; anti-inflammatory and local anesthetic; presents micromolar affinity at brain aBungarotoxin-sensitive nAChR.

Alkaloid C₃₀H₄₂O₇N₂ from plants of the Aconitum genus, Ranunculaceae.

• Molecular Weight : 542 Da.
  
  
• Melting Point : 208-210°C.
  
  
• Solubility in : chloroform; less in methanol, ethanol, acetone and water.
  
  
• Purity min. : 97 %.
  
  
• Biological Activity : N-Desacetyl lappaconitine 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-Desacetyl lappaconitine 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-Desacetyl lappaconitine acts as a local anaesthetic and as an anti-inflammatory.
  
  
• Toxicity (LD₅₀) : mice (i.v.): 7.5 mg/kg. mice (i.p.): 30.0 mg/kg. mice (orally): 82.0 mg/kg.
  
  
• Storage recommendations : Store at +4°C, in dark place.
  
  
• CAS Reg. No. : 11033-64-0
  
  
• Bibliography :
  
  1. Dzjakhangirov et al. Rept. Acad. Sci. UzSSR (1990) (Russian). 8:44-48