Eplerenone

Eplerenone, an aldosterone receptor antagonist similar to spironolactone, has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors. (In Vitro) :Eplerenone inhibits the human mineralocorticoid receptor with IC50 value of 0.081 μM. (In Vivo) :Eplerenone (oral, 200 mg/kg/day for 3 months) significantly reduces oxidative stress and atherosclerosis progression in atherosclerotic apolipoprotein edeficient (EO) mice.