Biochem/physiol Actions
PD-118057 is an activator of ether-a-go-go-related (hERG) potassium channel. PD-118057 is a second identified hERG channel activator, a representative in the series of structural analogs; PD-118057 at 10 μM leads to a 111% current increase in rabbit ventricular wedge (in comparison RPR260243 leads to only a 15% increase at the same concentration);PD-118057, unlike RPR260243, does not have a major effect on gating or kinetic properties of this channel. PD-118057prevents and reverses QT interval prolongation; Compounds such as PD-118057 may offer new approach in the treatment of delayed repolarization conditions, which occur in inherited or acquired long QT syndrome and congestive heart failure |