Eplerenone is a potassium-sparing diuretic that selectively blocks aldosterone activation of the mineralcorticoid receptor (IC50 = 122 nM), demonstrating little activity towards other steroid receptors (IC50 > 9 µM for glucocorticoid, androgen, progesterone, and estrogen receptors), and is indicated for the treatment of hypertension and heart failure.
Eplerenone/依普利酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
SU-5416/hypoxia-induced PAH model
Chow supplementation
0.6 mg/1g chow
Starting immediately after SU-5416 administration and continued for 21 days
To assess the effect of Eplerenone on PAH, results showed that Eplerenone significantly attenuated pulmonary hypertension and pulmonary vascular fibrosis.
Circulation. 2014 Jul 8;130(2):168-79
Mice
Obese diabetic db/db mice
Chow
100 mg/kg/day
Once daily for 16 weeks
To evaluate the effect of Eplerenone on the expression of inflammatory factors, adiponectin, and PPARγ in adipose tissue and heart of obese diabetic mice. Results showed that Eplerenone reduced the expression of TNF-α, MCP-1, PAI-1, and CD68 in adipose tissue, and increased the expression of adiponectin and PPARγ in adipose tissue and heart.
Circulation. 2008 Apr 29;117(17):2253-61.
Mice
Aldosterone infusion model
Oral gavage
100 mg/kg/d
Once daily for 14 days
Eplerenone rescued aldosterone-induced EPC dysfunction, impaired vascularization, and endothelial dysfunction via MR blockade, independent of blood pressure effects.
Eur Heart J. 2011 May;32(10):1275-86.
C57BL/6 mice
High-fat diet-induced obesity model
Oral
200 mg/kg/day
Once daily for 14 weeks
To evaluate the effect of eplerenone on obesity-induced endothelial dysfunction. Results showed that eplerenone treatment prevented the impairment of endothelium-dependent relaxation caused by obesity.
Eur Heart J. 2013 Dec;34(45):3515-24
C57Bl/6J mice
Carfilzomib-induced nephrotoxicity model
Oral
165 mg/kg
Daily administration for 6 days
To evaluate the protective effect of Eplerenone on Carfilzomib-induced nephrotoxicity, it was found that Eplerenone partially prevented the Carfilzomib-induced increase in creatinine and BUN, and restored urine volume, glomerular volume, and Lcn2 levels.
Hemasphere. 2022 Oct 18;6(11):e791.
Mice
Kcnmb1/H11002//H11002 mice
Oral
100 mg/kg BW/day
Once daily for 10 days
To investigate the effect of Eplerenone on hypertension and fluid balance in Kcnmb1/H11002//H11002 mice. Results showed that Eplerenone corrected the fluid imbalance and significantly reduced hypertension.
Proc Natl Acad Sci U S A. 2009 Jul 14;106(28):11800-5
Eplerenone/依普利酮 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
293 cells
Function assay
16 h
Displacement of [3H]aldosterone from human mineralocorticoid receptor expressed in 293 cells after 16 hrs by scintillation counting, IC50=2.6 μM
25187277
COS1 cells
Function assay
1 days
Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay, IC50=1.3 μM
22074142
Huh7 cells
Function assay
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay, IC50=0.122 μM
搜索
