Effect of SEA0400, a novel inhibitor of sodium‐calcium exchanger, on myocardial ionic currents

• Hikaru Tanaka

• Kazuhide Nishimaru

• Tokiko Aikawa

• Wataru Hirayama

• Yoshio Tanaka

• Koki Shigenobu

Abstract

The effects of 2‐[4‐[(2,5‐difluorophenyl) methoxy]phenoxy]‐5‐ethoxyaniline (SEA0400), a newly synthesized Na + ‐Ca 2+ exchanger (NCX) inhibitor, on the NCX current and other membrane currents were examined in isolated guinea‐pig ventricular myocytes and compared with those of 2‐[2‐[4‐(4‐nitrobenzyloxy) phenyl]ethyl]isothiourea (KB‐R7943). SEA0400 concentration‐dependently inhibited the NCX current with a 10 fold higher potency than that of KB‐R7943; 1 μ M SEA0400 and 10 μ M KB‐R7943 inhibited the NCX current by more than 80%. KB‐R7943, at 10 μ M , inhibited the sodium current, L‐type calcium current, delayed rectifier potassium current and inwardly rectifying potassium current by more than 50%, but SEA0400 (1 μ M ) had no significant effect on these currents. These results indicate that SEA0400 is a potent and highly selective inhibitor of NCX, and would be a powerful tool for further studies on the role of NCX in the heart and the therapeutic potential of its inhibition. British Journal of Pharmacology (2002) 135 , 1096–1100; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0704574">10.1038/sj.bjp.0704574

Journal

• British Journal of Pharmacology

  British Journal of Pharmacology 135 (5), 1096-1100, 2002-03

  Wiley

Keywords

• Pharmacology

Details

• CRID: 1360292621309542272
• NII Article ID: 80015264044
• DOI: 10.1038/sj.bjp.0704574
• ISSN: 14765381
• ISSN: 00071188
• ISSN: http://id.crossref.org/issn/00071188
• Web Site: https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1038%2Fsj.bjp.0704574
• Web Site: https://bpspubs.onlinelibrary.wiley.com/doi/pdf/10.1038/sj.bjp.0704574
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