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

Research output: Contribution to journalArticle

63 Citations (Scopus)

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
StatePublished - Mar 17 1999

Fingerprint

Tacrine
Brain
Butyrylcholinesterase
Cholinesterase Inhibitors
Acetylcholinesterase
Palliative Care
Inhibitory Concentration 50
Oral Administration
1,7-N-heptylene-bis-9,9'-amino-1,2,3,4-tetrahydroacridine
Pharmaceutical Preparations

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., ... Han, Y. F. (1999). Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE. NeuroReport, 10(4), 789-793.

Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE. / Wang, Hong; Carlier, Paul R.; Ho, Wing Lok; Wu, Dong Cheng; Lee, Nelson Tze Kin; Li, Crystal P L; Pang, Yuan-Ping; Han, Yi Fan.

In: NeuroReport, Vol. 10, No. 4, 17.03.1999, p. 789-793.

Research output: Contribution to journalArticle

Wang, H, Carlier, PR, Ho, WL, Wu, DC, Lee, NTK, Li, CPL, Pang, Y-P & Han, YF 1999, 'Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE', NeuroReport, vol. 10, no. 4, pp. 789-793.
Wang H, Carlier PR, Ho WL, Wu DC, Lee NTK, Li CPL et al. Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE. NeuroReport. 1999 Mar 17;10(4):789-793.
Wang, Hong ; Carlier, Paul R. ; Ho, Wing Lok ; Wu, Dong Cheng ; Lee, Nelson Tze Kin ; Li, Crystal P L ; Pang, Yuan-Ping ; Han, Yi Fan. / Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE. In: NeuroReport. 1999 ; Vol. 10, No. 4. pp. 789-793.
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