a medium-lasting and selective M₂ muscarinic receptors antagonist (potency is intermediate between that of L60 08 Imperialine and L60 32/L60 33 chloro-Imperialines).

Alkaloid C₂₇H₄₁NO₃ derivative of Imperialine extracted from Petilium eduardi.

• Molecular Weight : 427 Da.
  
  
• Melting Point : 228-235 °C.
  
  
• Solubility in : dissolves well in chloroform, slightly in methanol and ethanol, not well in acetone.
  
  
• Purity min. : 97% (TLC).
  
  
• Biological Activity : presents a M₂-selective activity: ED50 on rats under anaesthesia (i.v.) is 0.019 mg/kg (77.5% of Atropine activity). On the other muscarinic receptor subtypes, the effects of Imperialone are the following: - M4 receptors from rat intestine, EC50 = 7.4 10-8 g/ml (4.8% of Atropine activity). - M3 receptors from rat salivary glands, ED50 = 16.2 mg/kg (0.027 % of Atropine activity). Imperialone is more potent and presents a 3 to 5 times longer M₂ cholinoblocking effect than L60 08 Imperialine at similar concentration. Therefore, it can be considered as a medium-acting cholinoblocker.
  
  
• Toxicity (LD₅₀) : mice (i.v.): 44 mg/kg. (36-52)
  
  
• Storage recommendations : Store at +4°C, in dark place.
  
  
• CAS Reg. No. : 61989-75-1
  
  
• Bibliography :
  
  1. Nurridinov et al., Chem. Nat. Comp. (1968). 333
  2. Mirzaev, unbublished results.