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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

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

The anticholinesterase effects of bis(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 dose-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.[1]

References

  1. Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE. Wang, H., Carlier, P.R., Ho, W.L., Wu, D.C., Lee, N.T., Li, C.P., Pang, Y.P., Han, Y.F. Neuroreport (1999) [Pubmed]
 
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