Description
Ro 46-2005 is the first synthetic orally active nonpeptide antagonist of endothelin receptor with equipotent potency (IC50=0.2-0.5uM) for ETA and ETB; has no effect on plasma concentrations of big ET-1 and only a minor effect on those of ET-3; sufficient to inhibit the pressor effect of the precursor big ET-1 at much lower doses (1 to 10mg/kg i.v.). Hypertension Preclinical