Description
Eplerenone displays antihypertensive, anti-inflammatory, and anti-angiogenic activities; it inhibits the mineralocorticoid receptor. Eplerenone inhibits aldosterone-induced expression of COX (therefore decreasing PGE2 levels), preventing the induction of COX and resulting kidney damage in high salt diets. This compound also prevents salt-induced increases in NOX expression, decreasing oxidative stress in the kidney as well. In spontaneously hypertensive rats, eplerenone inhibited cardiac remodeling (hypertrophy) and left ventricle dysfunction. The antiangiogenic activity of eplerenone is characterized by its inhibition of VEGF expression in the kidney.
References
Yasuoka S, Kai H, Kajimoto H, et al. Blood pressure variability activates cardiac mineralocorticoid receptor and induces cardiac remodeling in hypertensive rats. Circ J. 2013;77(6):1474-81. PMID: 23470864.
Bayorh M, Rollins-Hairston A, Adiyiah J, et al. Eplerenone inhibits aldosterone-induced renal expression of cyclooxygenase. J Renin Angiotensin Aldosterone Syst. 2012 Sep;13(3):353-9. PMID: 22554826.
Bayorh MA, Rollins-Hairston A, Adiyiah J, et al. Eplerenone suppresses aldosterone/ salt-induced expression of NOX-4. J Renin Angiotensin Aldosterone Syst. 2011 Sep;12(3):195-201. PMID: 21292834.
Eatman D, Layas MF, Bayorh MA. Eplerenone Suppresses Salt-Induced Vascular Endothelial Growth Factor Expression in the Kidney. Kidney Blood Press Res. 2010 Jun 23;33(3):167-173. PMID: 20571278.
