Antagonists of the Mineralocorticoid Receptor or A New Pharmacological Class?

Milla Marques Hermidorff,Leonardo Vinícius Monteiro De Assis,Mauro César Isoldi

doi:10.4172/2157-7013.1000222

Abstract

Antagonists of the Mineralocorticoid Receptor or A New Pharmacological Class?

Highlights

A reduction in the blood pressure levels triggers, among other responses, a signaling cascade mainly controlled by the kidneys; this event is responsible for reestablishing the blood pressure, being known as renin, angiotensin, and aldosterone system – RAAS
Most of the effects displayed by aldosterone are attributed to its binding to the mineralocorticoid receptor (MR); this receptor is localized in the cytoplasm in a perinuclear region
It was speculated that this nonspecific binding to the MR displayed by spironolactone could be related, at the least in some part, to its cardioprotective effects; this was disregarded with the development of eplerenone – an MR antagonist with low affinity but with a higher selectivity over the MR, which leads to reduced sexual side effects [11]

Summary

Introduction

A reduction in the blood pressure levels triggers, among other responses, a signaling cascade mainly controlled by the kidneys; this event is responsible for reestablishing the blood pressure, being known as renin, angiotensin, and aldosterone system – RAAS. The aldosterone, the last hormone released in this cascade, displays several effects in its target tissue such as kidneys, colon, brain, and cardiovascular system [1]; high levels of aldosterone, in certain diseases, lead to deleterious effects in most of these organs.

Results

Conclusion