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Tacrine is a derivative of aminoacridine which functions as an inhibitor of both AChE and butyrylcholinesterase.1 It has been used clinically in the treatment of Alzheimer’s disease.2,3 Tacrine also inhibits the uptake of serotonin and noradrenaline in rat cerebral cortex2,4 and decreases depolarization-induced calcium influx through L-type calcium channels in SN56 neuronal cells.5
1
Crismon, M.L. Pharmacokinetics and drug interactions of cholinesterase inhibitors administered in Alzheimer’s disease. Pharmacotherapy1847-54(1998).
2
Drukarch, B., Leysen, J.E., and Stoof, J.C. Further analysis of the neuropharmacological profile of 9-amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer’s disease. Life Sci421011-1017(1988).
3
Giacobini, E. Cholinesterase inhibitors for Alzheimer’s disease therapy: From tacrine to future applications. Neurochem Int32413-419(1998).
4
McKenna, M.T., Proctor, G.R., Young, L.C., et al. Novel tacrine analogues for potential use against Alzheimer’s disease: Potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. J Med Chem403516-3523(1997).
5
Dolezal, V., Lisá, V., and Tucek, S. Effect of tacrine on intracellular calcium in cholinergic SN56 neuronal cells. Brain Res769219-224(1997).
Drukarch, B., Leysen, J.E., and Stoof, J.C. Further analysis of the neuropharmacological profile of 9-amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer’s disease. Life Sci421011-1017(1988).
Giacobini, E. Cholinesterase inhibitors for Alzheimer’s disease therapy: From tacrine to future applications. Neurochem Int32413-419(1998).
McKenna, M.T., Proctor, G.R., Young, L.C., et al. Novel tacrine analogues for potential use against Alzheimer’s disease: Potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. J Med Chem403516-3523(1997).
Crismon, M.L. Pharmacokinetics and drug interactions of cholinesterase inhibitors administered in Alzheimer’s disease. Pharmacotherapy1847-54(1998).
Dolezal, V., Lisá, V., and Tucek, S. Effect of tacrine on intracellular calcium in cholinergic SN56 neuronal cells. Brain Res769219-224(1997).