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  • 标题:Metabolism of Mutagenicity-Deprived 3-Fluoroquinoline : Comparison with Mutagenic Quinoline
  • 本地全文:下载
  • 作者:Ken-ichi SAEKI ; Kazuhiko TAKAHASHI ; Yutaka KAWAZOE
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1993
  • 卷号:16
  • 期号:3
  • 页码:232-234
  • DOI:10.1248/bpb.16.232
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:3-Fluorinated quinoline (3FQ), a non-mutagenic derivative of the potent mutagen quinoline, was metabolized with a microsomal enzyme fraction isolated from the 3-methylcholanthrene-treated rat liver. The metabolites were 3-fluoro-5, 6-dihydroquinoline-5, 6-trans-diol (72%), 3-fluoroquinoline 1-oxide (6%), 3-fluoro-5, 6-dihydroquinoline-5, 6-cis-epoxide (1%), and 4 unidentified metabolites (11%). Since this metabolic pattern is similar to that obtained with unfluorinated quinoline, the epoxidation of the benzene moieties of quinoline and 3-fluoroquinoline is most likely a detoxication process and not mutagenic activation.
  • 关键词:fluoroquinoline;quinoline;metabolism;microsomal oxidation;mutagenicity
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