Mineralocorticoid receptor (MR) antagonism has proven to effectively attenuate the pathophysiological effects of aldosterone in clinical and experimental settings of hypertension and heart failure. MR activates transcription of target genes upon aldosterone binding, and eplerenone selectively binds to MR and blocks aldosterone- mediated activation. In this review, we summarize the preclinical and clinical evidence supporting the beneficial effects of eplerenone (INSPRATM), a selective aldosterone blocker, in the treatment of hypertension and heart failure. We also review the current status in understanding the molecular mechanisms of action of the MR and its ligand. In addition, we compare the effects of eplerenone and spironolactone, a nonselective aldosterone blocker, on the transcriptional activity of MR and provide a molecular explanation for the improved side-effect profile of eplerenone compared with spironolactone.
Keywords: hypertension, reninangiotensin-aldosterone system, angiotensin-converting enzyme, aldosterone antagonist., antihypertensive, histone acetyltransferase, cortical collecting tubule
Monitoring Calcific Aortic Valve Disease: The Role of Biomarkers
Current Medicinal Chemistry The Role of Angiotensin Type 1 Receptor in Inflammation and Endothelial Dysfunction
Recent Patents on Cardiovascular Drug Discovery (Discontinued) Emerging Roles for Connexins in Hypertension
Current Hypertension Reviews Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets?
Current Molecular Pharmacology Endothelin-1-Induced Signaling Pathways in Vascular Smooth Muscle Cells
Current Vascular Pharmacology Mechanistic Considerations on the Development of Lung Edema: Vascular, Perivascular and Molecular Aspects from Early Stage to Tissue and Vascular Remodeling Stage
Current Respiratory Medicine Reviews Repurposing of Existing Drugs for the Bacterial Infections: An In silico and In vitro Study
Infectious Disorders - Drug Targets Pulmonary Hypertension: Types and Treatments
Current Cardiology Reviews Magnetic Resonance Imaging Findings of Sixth Cranial Nerve Palsies in Patients Presenting with Diplopia
Current Medical Imaging Endothelin Receptor Antagonists as Disease Modifiers in Systemic Sclerosis
Inflammation & Allergy - Drug Targets (Discontinued) Arterial Stiffness As A Therapeutic Target For Isolated Systolic Hypertension: Focus on Vascular Calcification and Fibrosis
Current Hypertension Reviews Evaluation of Clinical Efficacy of Fasudil for the Treatment of Pulmonary Arterial Hypertension
Recent Patents on Cardiovascular Drug Discovery (Discontinued) Cryptogenic Liver Diseases: Sailing by Sight from HIV Co-Infection with Hepatitis Viruses to HIV Mono-Infection Through the Pillars of Hercules
Current HIV Research Can Life Before Birth Affect Health Ever After?
Current Women`s Health Reviews Riboregulators and Metabolic Disorders: Getting Closer Towards Understanding the Pathogenesis of Diabetes Mellitus?
Current Molecular Medicine Anti-Inflammatory, Gastrointestinal and Hepatoprotective Effects of Ocimum sanctum Linn: An Ancient Remedy with New Application
Inflammation & Allergy - Drug Targets (Discontinued) Medicinal Plants with Multiple Effects on Cardiovascular Diseases: A Systematic Review
Current Pharmaceutical Design Aldosterone to Renin Ratio (ARR) in Clinical use, with Reference to the Primary Care Setting: ARR to Whom, When, How, What for?
Current Hypertension Reviews Medical Management of the Diabetic Patient with Coronary Artery Disease
Current Pharmaceutical Design The Role of Angiotensin in Obesity and Metabolic Disease
Endocrine, Metabolic & Immune Disorders - Drug Targets