New Benzodiazepines Alter Acetylcholinesterase and ATPDase Activities |
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Authors: | Maria R C Schetinger Neuza M Porto Maria B Moretto Vera M Morsch João Batista T da Rocha Vânia Vieira Franciele Moro Roseli Tatto Neis Sandra Bittencourt Hélio G Bonacorso Nilo Zanatta |
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Institution: | (1) Departamento de Química, Centro de Ciências Naturais e Exatas, Brazil;(2) Departamento de Ciências Biológicas, Centro de Educação, Ciências Biológicas e Artes, Universidade da Região da Campanha, 97300-000 São Gabriel, RS, Brasil;(3) Departamento de Análises Clinicas, Centro de Ciências da Saúde, Universidade Federal de Santa Maria, 97105-900 Santa Maria, RS, Brasil;(4) Departamento de Química, Centro de Ciências Naturais e Exatas, Brazil |
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Abstract: | This study examines the effect of new 1,5 benzodiazepines on acetylcholinesterase (AChE) and ATPDase (apyrase) activities from cerebral cortex of adult rats. Simultaneously, the effects of the classical 1,4-benzodiazepine on these enzymes were also studied for comparative purpose. The compounds 2-trichloromethyl-4-phenyl-3H-1,5-benzodiazepin and 2-trichloromethyl-4-(p-methyl-phenyl)-3H-1,5-benzodiazepin significantly inhibited acetylcholinesterase activity (p < 0.01) when tested in the range of 0.18–0.35 mM. The inhibition caused by these two new benzodiazepines was noncompetitive in nature. Similarly, at concentrations ranging from 0.063 to 0.25 mM, the 1,5 benzodiazepines inhibited ATP and ADP hydrolysis by synaptosomes from cerebral cortex (p < 0.01). However, the inhibition of nucleotide hydrolysis was uncompetitive in nature. Our results suggest that, although diazepam and the new benzodiazepines have chemical differences, they both presented an inhibitory effect on acetylcholinesterase and ATPDase activities. |
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Keywords: | Benzodiazepines acetylcholinesterase ATPDase cerebral cortex |
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