Rostafuroxin is an antihypertensive compound and a Na,K-ATPase antognist which displaces [3H]ouabain from the dogkidney Na+,K+-ATPase with IC50 of 1.5 nM.
Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na+,K+-ATPase (ATP1A1) antognist[3]. Rostafuroxin (PST 2238) is a new oral antihypertensive agent able to selectively antagonize EO, adducin pressor, and molecular effects. It is endowed with high potency and efficacy in reducing blood pressure and preventing organ hypertrophy in animal models representative of both adducin and EO mechanisms. In the vasculature, it normalizes the increased myogenic tone caused by nanomolar ouabain[4]. The antihypertensive rostafuroxin suppresses Na(+) resorption and the Src-epidermal growth factor receptor-ERK pathway in kidney tubule cells[5]. In A549 cells and HSAEC, RSV (Human respiratory syncytial virus) uptake could be inhibited by the cardiotonic steroid ouabain and the digitoxigenin derivative PST2238 (rostafuroxin) that bind specifically to the ATP1A1 extracellular domain and block RSV-triggered EGFR (epidermal growth factor receptor) Tyr845 phosphorylation[6].
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