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  • 标题:No Inhibition of Cytochrome P450 Activities in Human Liver Microsomes by Sulpiride, an Antipsychotic Drug
  • 本地全文:下载
  • 作者:Toshiro Niwa ; Sachiko Inoue ; Toshifumi Shiraga
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2005
  • 卷号:28
  • 期号:1
  • 页码:188-191
  • DOI:10.1248/bpb.28.188
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The effects of sulpiride, an antipsychotic drug, on cytochrome P450 (CYP) activities in human liver microsomes were investigated. Sulpiride at 50 or 500 μ M concentration neither inhibited nor stimulated CYP1A2-mediated 7-ethoxyresorufin O -deethylation, CYP2C9-mediated tolbutamide hydroxylation, CYP2C19-mediated S -mephenytoin 4′-hydroxylation, CYP2D6-mediated debrisoquine 4-hydroxylation, CYP2E1-mediated chlorzoxazone 6-hydroxylation, CYP3A4-mediated nifedipine oxidation, or CYP3A4-mediated testosterone 6β-hydroxylation. The free fractions of sulpiride in the incubation mixture estimated by ultracentrifugation were more than 90.5%. These results suggest that sulpiride would not cause clinically significant interactions with other drugs, which are metabolized by CYPs, via the inhibition of metabolism.
  • 关键词:sulpiride;antipsychotic drug;human liver microsomes;cytochrome P450;drug interaction
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