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 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.
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 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 .
The small molecule SEA0400 is an inhibitor of which ion antiporter/exchanger?
The small molecule SEA0400 is an inhibitor of which ion antiporter / exchanger ?
NCX
Na(+)/Ca(2+) exchanger NCX