a nicotinic receptor antagonist at the neuromuscular junction; ganglioblocker; potent medium-acting muscle relaxant and hypotensive.

C₁₉-norditerpenoid alkaloid C₃₆H₄₈N₂O₁₀.HClO₄ purified from plants of the Aconitum genus, Ranunculacae.

• Molecular Weight : 768 Da.
  
  
• Melting Point : 184-186 °C (ethanol; forming foam); softens at 170°C.
  
  
• Solubility in : moderately in water and methanol; not well in ethanol.
  
  
• Purity min. : IR, NMR, TLC [aluminium oxide, benzene:ethanol (20:1)], TLC [silicagel, benzene:ethanol (9:1) ], melting point.
  
  
• Physical Form : cream-white crystal.
  
  
• Biological Activity : Good penetration of the blood-tissue barrier. Acts on nicotinic cholinoreceptors of the Peripheral and Central Nervous Systems, whatever the way of administering in vivo.
  On cat under anaesthesia, 1.5 mg/kg (i.v.) or 30 mg/kg (orally) block the activity of N-cholinoreceptors at the neuromuscular junction.10-5 g/ml block the neuromuscular transmission on the rat diaphragm preparation.
  0.5-2 mg/kg (i.v.) on cat under anaesthesia, cause hypotension due to the blockade of the transmission of nervous impulses in sympathetic and orthosympathetic ganglia.
  Belongs to the family of non depolarizing myorelaxant. Antagonists: Proserine, Galanthamine.
  
  
• Toxicity (LD₅₀) : mice (orally) : 31 mg/kg. mice (i.v.) : 2.6 mg/kg. mice (i.p.): 12.5 mg/kg.
  
  
• Storage recommendations : Stable in dry state, store at + 4°C, in dark place. Solution for experiments in vitro: 10-5 - 10-7 M; doses for experiments in vivo on cats and dogs: 1-3 mg/kg (i.v.) or 20-30 mg/kg (orally).
  
  
• CAS Reg. No. : 321938-55-0
  
  
• Bibliography :
  
  1. Pelletier et al., J. Am. Chem. Soc.(1981) 103:6536-6538
  2. Shamma et al., J. Nat. Prod. (1979). 42:615-623
  3. Djahangirov, "About the pharmacology of the alkaloid Lycaconitine." Problems of Pharmacology and Pharmacy, Tashkent (1976) (Russian). 4: 21-22