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  • 标题:Hirsutenone Directly Blocks Human ether-a-go-go Related Gene K+ Channels
  • 本地全文:下载
  • 作者:Jihyun Yun ; Hyemi Bae ; Sun Eun Choi
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2011
  • 卷号:34
  • 期号:12
  • 页码:1815-1822
  • DOI:10.1248/bpb.34.1815
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The aim of the present study was to investigate whether hirsutenone affects the human ether-a-go-go related gene (hERG) K+ channels. Many drugs promote formation of the acquired form of long QT syndrome (LQTS) by blocking the hERG K+ channels. Hirsutenone, a new candidate for the treatment inflammatory skin lesions, induced a concentration-dependent decrease in hERG K+ current amplitudes. Hirsutenone significantly decreased the time constants at the onset of inactivation. However, the reductions in the time constants of steady-state inactivation and the recovery from inactivation after hirsutenone treatment were not significant. In addition, the drug had no effect on the voltage-dependent activation curve or the steady-state inactivation curve. In summary, hirsutenone potentially acts as a blocker of hERG K+ channels functioning by modifying the channel inactivation kinetics.
  • 关键词:human ether-a-go-go related gene;hirsutenone;long QT syndrome;patch clamp
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