Effects of KRN4884, a Novel K^+ Channel Opener, on Ionic Currents in Rabbit Femoral Arterial Myocytes

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著者

    • Sasaoka Akiko SASAOKA Akiko
    • Department of Molecular and Cellular Pharmacology, Graduate School of Pharmaceutical Sciences, Nagoya City University
    • WATANABE Minoru
    • Department of Molecular and Cellular Pharmacology, Graduate School of Pharmaceutical Sciences, Nagoya City University
    • IMAIZUMI Yuji
    • Department of Molecular and Cellular Pharmacology, Graduate School of Pharmaceutical Sciences, Nagoya City University

抄録

Effects of KRN4884 (5-amino-<i>N</i>-[2-(2-chlorophenyl)ethyl]-<i>N'</i>-cyano-3-pyridinecarboxamidine), a novel K<sup>+</sup> channel opener, on ionic currents were examined in rabbit femoral arterial myocytes (RFAMs). Under whole-cell clamp conditions where cells were superfused with 5.9 mM K<sup>+</sup> bathing solution, KRN4884 elicited an outward current at −30 mV. KRN4884-induced current had a reversal potential of −78 mV and was abolished by application of glibenclamide (glib). KRN4884 was approximately 43 times more potent than levcromakalim in activating an ATP-sensitive K<sup>+</sup> current (I<sub>K-ATP</sub>). On the other hand, KRN4884 affected neither voltage-dependent Ca<sup>2+</sup> nor delayed rectifier K<sup>+</sup> channel currents. In the inside-out patch clamp configuration where cells were superfused with the symmetrical 140 mM K<sup>+</sup> solution, KRN4884 activated 47 pS K<sup>+</sup> channels in the presence of adenosine diphosphate. Similar 47 pS K<sup>+</sup> channels, which were reversibly inhibited by glib, were recorded under outside-out patch conditions. Using RT-PCR analysis, we found that inward rectifier K channel 6.1 (Kir6.1) and sulfonylurea 2B (SUR2B) transcripts were predominantly expressed in rabbit femoral artery. These results indicate that KRN4884 potently activates I<sub>K-ATP</sub> in RFAMs. The KRN4884-sensitive 47 pS K<sup>+</sup> channel activity underlying I<sub>K-ATP</sub> is a vascular type K<sub>ATP</sub> channel consisting of Kir6.1 and SUR2B and has similar characteristics to those of ATP-sensitive K<sup>+</sup> channels activated by K<sup>+</sup> channel openers in other types of smooth muscles.<br>

収録刊行物

  • Journal of pharmacological sciences

    Journal of pharmacological sciences 93(3), 289-298, 2003-11-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10012544997
  • NII書誌ID(NCID)
    AA11806667
  • 本文言語コード
    ENG
  • 資料種別
    ART
  • ISSN
    13478613
  • NDL 記事登録ID
    6757891
  • NDL 雑誌分類
    ZS51(科学技術--薬学)
  • NDL 請求記号
    Z53-D199
  • データ提供元
    CJP書誌  CJP引用  NDL  J-STAGE 
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