Abstract

A potent and specific Na+/Ca2+ exchange (NCX) inhibitor would be very useful not only for studying the physiological roles of NCX but also for potentially offering a new drug therapy for cardiovascular diseases and so on. We here examined electrophysiological properties of YM-244769, a novel benzyloxyphenyl NCX inhibitor, using the whole-cell voltage-clamp technique. Inward and outward NCX currents (INCX) were measured in single cardiac ventricular myocytes of guinea pig. YM-244769 efficiently suppressed the uni-directional outward INCX with the IC50 value of 0.05 μM, whereas the blocking effect on the uni-directional inward INCX was less potent (IC50=about 10 μM).

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