a nicotinic AChR antagonist. Potent short-acting ganglioblocker. Hypotensive. Weak penetration of biological membranes - quaternary analog of Temechine.

Quinicludine derivative, C₁₂H₂₄IN, synthetic.

• Molecular Weight : 309.23 Da.
  
  
• Melting Point : 238-242 °C.
  
  
• Solubility in : water, ethanol, chloroform.
  
  
• Purity min. : min. 99.5%.
  TLC (Silufol UV-254, MeOH:NH3(25%) Rf <0.1, development with Dragendorff¨ reagent); NMR (D2O).
  
  
• Physical Form : colorless crystal powder.
  
  
• Chemical Name : 1,2,2,6,6-pentamethylquinicludinium iodide.
  
  
• Biological Activity : Nicotinic AChR antagonist. Potent short-acting ganglioblocker.
  
  Weak penetration of biological membranes. Quaternary analog of Temechine and Pempidine. Stable bicyclic analog of the very unstable quaternary salts of Pempidine.
  
  Short-acting hypotensive (4-20 min) used in surgery for obtaining hypotension of the desired level and duration [1-5]. In contrast to Arphonad has no histamine-like activity and direct vasodilatory action. Less toxic than Arphonad [1].
  
  In clinical practice besides surgery is used for treament of pulmonary or cervical edemas and chronical hypertension caused by acute renal deficiency. Marked absence of tachicardia and prolongation of myorelaxant action of other drugs.
  
  For infusions are used 0.01-0.05% solutions in isotonic NaCl.
  
  
• Toxicity (LD₅₀) : mice (orally): 275 mg/kg.
  
  
• Storage recommendations : store at room temperature in a dark place. Solution for use: dissolve in water: 10-3M (2 mg in 6.47 ml), stable for 1-2 days at 20°C.
  
  
• Safety recommendations : do not swallow or inhale; avoid eye and skin contact.
  
  
• CAS Reg. No. : 41663-80-3
  
  
• Bibliography :
  
  1. Nikitskaya E.S. et al., Khim. Farm. Zh. (1974) (Russian) (8):59-60
  2. Sharapov I.M., Farm, Toksikol. (1974). (Russian). (1):25-29
  3. Parshin V.A., Khim-Pharm. Zh. (1977) (Russian). (6):143-147
  4. Bunatyan A.A. et al., Grekov Vestnik Chirurgii (Grekov Surgery Reports) (1971) (Russian). (6):121-122
  5. Mashkovsky M.D. et al., "Further developments in research on the chemistry and pharmacology of synthetic quinuclidine derivatives." Progr. Drug. Res., (1983). 27:9-61