an inhibitor of high-affinity choline uptake (HAChU) in synaptosomes; acetylcholine synthesis inhibitor; good penetration of biological membranes.

Quinicludine derivative, C₁₄H₁₄NOCl .HCl, synthetic.

• Molecular Weight : 284.18 Da.
  
  
• Melting Point : 185-187 °C.
  
  
• Solubility in : water, ethanol and DMSO.
  
  
• Purity min. : min. 99.5%.
  TLC [Silufol UV-254, MeOH:NH3(25%) Rf =0.68, development in UV light followed with Dragendorff¨ reagent]; NMR (D2O).
  
  
• Physical Form : slightly yellowish crystal powder.
  
  
• Chemical Name : Z-2-((3'chlorophenyl)methylene]-3-quinuclidon HCl;
  Z-2-[(3'-chlorophenyl)methylene]-3-oxoquinuclidine HCl
  
  
• Biological Activity : Cell permeable inhibitor of high-affinity choline uptake (HAChU). For comparative information see the attached table.
  good penetration of biological membranes.
  
  
• Toxicity (LD₅₀) : mice (orally) >700 mg/kg
  
  
• Storage recommendations : Store in a dark place in a dessicator; solutions are stable for 1-2 days at room temperature. Solution for use: 10-³ M (2 mg in 8.06 ml).
  
  
• Bibliography :
  
  1. Dahlbom R. et al., "Cell Mol. Basis Cholinergic Funct.", Dowdall M. J. and Hawthorne J. N. Eds., Horwood, Chichester U.K., (1987) 347-354
  2. Sterling et al., "Inhibition of high-affinity choline uptake and acetylcholine synthesis by quinuclidinyl and hemicholinium derivatives", J. Neurochem.(1986). 46(14):1170-1175
  3. Doukas P.H. et al., ibid, 355-360
  4. Baltzod F. et al., Biochem. Pharm. (1980). 29(18):2413-2416
  5. Tamaru M. et al., Brain Res (1988). 473(2):205-226
  6. Dowdall M.J. et al., in Cholinergic mechanisms and Psycopharmacology, Ed. D.J.Jenden, Plenum Press, N-Y, (1978). 359