Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE

Hong Wang, Paul R. Carlier, Wing Lok Ho, Dong Cheng Wu, Nelson Tze Kin Lee, Crystal P.L. Li, Yuan Ping Pang, Yi Fan Han

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63 Scopus citations

Abstract

The anticholinesterase effects of bls(7)-tacrine were compared with tacrine in vitro and in vivo. Based on IC50 ratios, the dimeric analog bis(7)-tacrine was, in a reversible manner, up to 150-fold more potent and 250-fold more selective than tacrine for acetylcholinesterase (ACHE) over butyrylcholinesterase (BChE). Following a single oral administration, both bis(7)-tacrine and tacrine produced close-dependent inhibitions of AChE in rat brain, but bis(7)-tacrine exhibited higher efficacy and AChE/BChE selectivity than tacrine. The anti-AChE efficacy of bis(7)-tacrine was quite similar following an oral or i.p. administration, but tacrine showed much lower efficacy when administered orally than when given i.p. These findings suggest bis(7)-tacrine, a highly potent and selective inhibitor of ACHE, can probably be used as an improved drug in the palliative treatment of AD.

Original languageEnglish (US)
Pages (from-to)789-793
Number of pages5
JournalNeuroReport
Volume10
Issue number4
DOIs
StatePublished - Mar 17 1999

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Keywords

  • Acetylcholinesterase
  • Alzheimer's disease
  • Bis(7)-tacrine
  • Cholinesterase inhibitor
  • Tacrine

ASJC Scopus subject areas

  • Neuroscience(all)

Cite this

Wang, H., Carlier, P. R., Ho, W. L., Wu, D. C., Lee, N. T. K., Li, C. P. L., Pang, Y. P., & Han, Y. F. (1999). Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE. NeuroReport, 10(4), 789-793. https://doi.org/10.1097/00001756-199903170-00023