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

Quinicludine derivative, C₈H₁₆INO, synthetic.

• Molecular Weight : 269.13 Da.
  
  
• Melting Point : >300 蚓.
  
  
• Solubility in : water, ethanol and DMSO.
  
  
• Purity min. : min. 99.5%. (NMR (D2O))
  
  
• Physical Form : slightly yellowish crystal powder.
  
  
• Chemical Name : 1-methyl-3-hydroxyquinuclidinium iodide.
  
  
• Biological Activity : Cell impermeable inhibitor of high-affinity choline uptake (HAChU). For comparative information see the attached table. Inhibits HAChU (1 然 of Choline) into Torpedo T-sacs: IC₅₀ = 8 然; Homocholine: IC₅₀ = 2 然; Thiocholine: IC₅₀ = 6 然; Acetylcholine: IC₅₀ = 10 然; TMA: IC₅₀ = 63 然; TEA: IC₅₀ = 132 然. In rat cortex synaptosomes: IC₅₀ = 72.0 然 [2]; Hemicholium-3: IC₅₀ = 0.06 然; Acetylsecohemicholinium-3: IC₅₀ = 0.64 然.
  
  40 % inhibition of ACh synthesis [2] (see comparative table).
  poor penetration of biological membranes.
  
  
• Toxicity (LD₅₀) : mice (orally) 400 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^-3M (2 mg in 7.43 ml).
  
  
• CAS Reg. No. : 6659-52-5
  
  
• 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