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, Yifan Han

Research output: Journal article publicationJournal articleAcademic researchpeer-review

69 Citations (Scopus)

Abstract

The anticholinesterase effects of bls(7)-tacrine were compared with tacrine in vitro and in vivo. Based on IC50ratios, 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
Pages (from-to)789-793
Number of pages5
JournalNeuroReport
Volume10
Issue number4
DOIs
Publication statusPublished - 17 Mar 1999
Externally publishedYes

Keywords

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

ASJC Scopus subject areas

  • Neuroscience(all)

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