論文

査読有り
2017年

Suppressive Effect of Carvedilol on Na+/Ca2+ Exchange Current in Isolated Guinea-Pig Cardiac Ventricular Myocytes

PHARMACOLOGY
  • Miyuki Tashiro
  • ,
  • Yasuhide Watanabe
  • ,
  • Tomomi Yamakawa
  • ,
  • Kanna Yamashita
  • ,
  • Satomi Kita
  • ,
  • Takahiro Iwamoto
  • ,
  • Junko Kimura

99
1-2
開始ページ
40
終了ページ
47
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1159/000450753
出版者・発行元
KARGER

Background and Aims: Carvedilol ((+/)-1-(carbazol4-yloxy)-34[2-(o-nnethoxyphenoxy)ethyliannino]-2-propa- nol), a beta-adrenoceptor-blocker, has multi-channel blocking and vasodilator properties. This agent dose-dependently improves left ventricular function and reduces mortality in patients with arrhythmia and chronic heart failure. However, the effect of carvedilol on the cardiac Na+/Ca2+ exchanger (NCX1) has not been investigated. Methods and Results: We examined the effects of carvedilol and metoprolol, 2 beta-blockers, on Na+/Ca2+ exchange current (I-NCX) in guineapig cardiac ventricular cells and fibroblasts expressing dog cardiac NCX1. Carvedilol suppressed INcx in a concentration dependent manner but metoprolol did not. IC50 values for the Ca2+ influx (outward) and efflux (inward) components of INcx were 69.7 and 61.5 mu mol/l, respectively. Carvedilol at 100 mu mol/l inhibited I-NCX in CCL39 cells expressing wild type NCX1 similar to mutant NCX1 without the intracellular regulatory loop. Carvedilol at 30 mu mol/l abolished ouabain-induced delayed afterdepolarizations. Conclusion: Carvedilol inhibited cardiac NCX in a concentration-dependent manner in isolated cardiac ventricles, but metoprolol did not. We conclude that carvedilol inhibits NCX1 at supratherapeutic concentrations. (C) 2016 S. Karger AG, Basel

リンク情報
DOI
https://doi.org/10.1159/000450753
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/27673688
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000393268700005&DestApp=WOS_CPL
ID情報
  • DOI : 10.1159/000450753
  • ISSN : 0031-7012
  • eISSN : 1423-0313
  • PubMed ID : 27673688
  • Web of Science ID : WOS:000393268700005

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