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Interfering with mineralocorticoid receptor activation: the past, present, and future

Aldosterone is a potent mineralocorticoid produced by the adrenal gland. Aldosterone binds to and activates the mineralocorticoid receptor (MR) in a plethora of tissues, but the cardiovascular actions of aldosterone are of primary interest clinically. Although MR antagonists were developed as antihy...

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Autor principal: Dorrance, Anne M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Faculty of 1000 Ltd 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4126546/
https://www.ncbi.nlm.nih.gov/pubmed/25165560
http://dx.doi.org/10.12703/P6-61
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author Dorrance, Anne M.
author_facet Dorrance, Anne M.
author_sort Dorrance, Anne M.
collection PubMed
description Aldosterone is a potent mineralocorticoid produced by the adrenal gland. Aldosterone binds to and activates the mineralocorticoid receptor (MR) in a plethora of tissues, but the cardiovascular actions of aldosterone are of primary interest clinically. Although MR antagonists were developed as antihypertensive agents, they are now considered to be important therapeutic options for patients with heart failure. Specifically, blocking only the MR has proven to be a difficult task because of its similarity to other steroid receptors, including the androgen and progesterone receptors. This lack of specificity caused the use of the first-generation mineralocorticoid receptor antagonists to be fraught with difficulty because of the side effects produced by drug administration. However, in recent years, several advances have been made that could potentially increase the clinical use of agents that inhibit the actions of aldosterone. These will be discussed here along with some examples of the beneficial effects of these new therapeutic agents.
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spelling pubmed-41265462014-08-27 Interfering with mineralocorticoid receptor activation: the past, present, and future Dorrance, Anne M. F1000Prime Rep Review Article Aldosterone is a potent mineralocorticoid produced by the adrenal gland. Aldosterone binds to and activates the mineralocorticoid receptor (MR) in a plethora of tissues, but the cardiovascular actions of aldosterone are of primary interest clinically. Although MR antagonists were developed as antihypertensive agents, they are now considered to be important therapeutic options for patients with heart failure. Specifically, blocking only the MR has proven to be a difficult task because of its similarity to other steroid receptors, including the androgen and progesterone receptors. This lack of specificity caused the use of the first-generation mineralocorticoid receptor antagonists to be fraught with difficulty because of the side effects produced by drug administration. However, in recent years, several advances have been made that could potentially increase the clinical use of agents that inhibit the actions of aldosterone. These will be discussed here along with some examples of the beneficial effects of these new therapeutic agents. Faculty of 1000 Ltd 2014-08-01 /pmc/articles/PMC4126546/ /pubmed/25165560 http://dx.doi.org/10.12703/P6-61 Text en © 2014 Faculty of 1000 Ltd http://creativecommons.org/licenses/by-nc/3.0/legalcode All F1000Prime Reports articles are distributed under the terms of the Creative Commons Attribution-Non Commercial License, which permits non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review Article
Dorrance, Anne M.
Interfering with mineralocorticoid receptor activation: the past, present, and future
title Interfering with mineralocorticoid receptor activation: the past, present, and future
title_full Interfering with mineralocorticoid receptor activation: the past, present, and future
title_fullStr Interfering with mineralocorticoid receptor activation: the past, present, and future
title_full_unstemmed Interfering with mineralocorticoid receptor activation: the past, present, and future
title_short Interfering with mineralocorticoid receptor activation: the past, present, and future
title_sort interfering with mineralocorticoid receptor activation: the past, present, and future
topic Review Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4126546/
https://www.ncbi.nlm.nih.gov/pubmed/25165560
http://dx.doi.org/10.12703/P6-61
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