SEA0400 (1 microM) inhibited the NCX current by >80% without significantly affecting other membrane currents, demonstrating 10-fold higher potency and greater selectivity than KB-R7943.
SEA0400 is a potent and highly selective inhibitor of the Na(+)-Ca(2+) exchanger, providing a powerful tool for studying the role of NCX in the heart.
Absolute Event Rate: 80% vs 80%
The effects of 2-4-[(2,5-difluorophenyl) methoxyphenoxy]-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) phenylethyl]isothiourea (KB-R7943). SEA0400 concentration-dependently inhibited the NCX current with a 10 fold higher potency than that of KB-R7943; 1 microM SEA0400 and 10 microM KB-R7943 inhibited the NCX current by more than 80%. KB-R7943, at 10 microM, inhibited the sodium current, L-type calcium current, delayed rectifier potassium current and inwardly rectifying potassium current by more than 50%, but SEA0400 (1 microM) 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.
Tanaka et al. (Fri,) reported a other. SEA0400 vs. KB-R7943 (10 microM) was evaluated on NCX current inhibition. SEA0400 (1 microM) inhibited the NCX current by >80% without significantly affecting other membrane currents, demonstrating 10-fold higher potency and greater selectivity than KB-R7943.
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