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.

Cell impermeable inhibitor of high-affinity choline uptake (HAChU). For comparative information see the attached table. Inhibits HAChU (1 µM of Choline) into Torpedo T-sacs: IC₅₀ = 8 µM; Homocholine: IC₅₀ = 2 µM; Thiocholine: IC₅₀ = 6 µM; Acetylcholine: IC₅₀ = 10 µM; TMA: IC₅₀ = 63 µM; TEA: IC₅₀ = 132 µM. In rat cortex synaptosomes: IC₅₀ = 72.0 µM [2]; Hemicholium-3: IC₅₀ = 0.06 µM; Acetylsecohemicholinium-3: IC₅₀ = 0.64 µM.


40 % inhibition of ACh synthesis [2] (see comparative table).

poor penetration of biological membranes.

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