Eplerenone (CGP 30083) is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease.

Aldosterone:0.36 μM

Eplerenone increases total vascular and luminal areas in swine without affecting the endothelial area. In canine models, it significantly reduces left ventricular end-diastolic wall stress. Eplerenone attenuates the rise in pulse pressure due to aldosterone (Aldo) in rats, normalizing the wall stress curve, mean cross-sectional area, and EIIIA fibronectin levels in Aldo-salt hypertensive rats. The compound upregulates diminished endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats, markedly improving glomerulosclerosis and proteinuria. In mice, daily administration of 200 mg/kg of Eplerenone significantly lowers systolic and diastolic blood pressures compared to controls and increases serum phosphatase activity.