Mineralocorticoid receptor antagonists: The evolution of utility and pharmacology

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15 صفحه اول

30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development

The cDNA of the mineralocorticoid receptor (MR) was cloned 30 years ago, in 1987. At that time, spirolactone, the first generation of synthetic steroid-based MR antagonists (MRAs), which was identified in preclinical in vivo models, had already been in clinical use for 30 years. Subsequent decades of research and development by Searle & Co., Ciba-Geigy, Roussel Uclaf and Schering AG toward iden...

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Mineralocorticoid receptor antagonists in dialysis patients

Mineralocorticoid receptor (MR) antagonists are known to have beneficial effects in patients with cardiovascular disease without renal failure. However, there have been few published studies on the effectiveness of MR antagonists in dialysis patients, and most of the studies were small-sized. The present review focuses on the effectiveness of MR antagonists and the risk of hyperkalemia in dialy...

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30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Evolution of the mineralocorticoid receptor: sequence, structure and function.

The mineralocorticoid receptor (MR) is descended from a corticoid receptor (CR), which has descendants in lamprey and hagfish, cyclostomes (jawless fish), a taxon that evolved at the base of the vertebrate line. A distinct MR and GR first appear in cartilaginous fishes (Chondrichthyes), such as sharks, skates, rays and chimeras. Skate MR has a strong response to corticosteroids that are mineral...

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Cardioprotective effects of mineralocorticoid receptor antagonists at reperfusion.

AIMS Pre-treatment with mineralocorticoid receptor (MR) antagonists is reported to reduce myocardial infarct size from ischaemia/reperfusion. Here, we tested whether the MR antagonists potassium canrenoate and eplerenone could protect in the more clinically relevant schedule of administration at the end of ischaemia. METHODS AND RESULTS In all models, hearts were subjected to 30 min regional ...

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ژورنال

عنوان ژورنال: Kidney International

سال: 2000

ISSN: 0085-2538

DOI: 10.1046/j.1523-1755.2000.00983.x