Effects of bis(7)-tacrine, a novel anti-Alzheimer's agent, on rat brain AChE.
Neuroreport
; 10(4): 789-93, 1999 Mar 17.
Article
en En
| MEDLINE
| ID: mdl-10208549
ABSTRACT
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.
Buscar en Google
Banco de datos:
MEDLINE
Asunto principal:
Acetilcolinesterasa
/
Tacrina
/
Encéfalo
/
Inhibidores de la Colinesterasa
/
Nootrópicos
/
Enfermedad de Alzheimer
Límite:
Animals
Idioma:
En
Año:
1999
Tipo del documento:
Article