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Description: Eplerenone (also known as CGP 30083, Inspra, SC-66110) is a potent and selective mineralocorticoid receptor antagonist with an IC50 of 0.36 uM, it blocks the action of aldosterone, used to control high blood pressure. Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice.
References: Hypertension. 2005 Apr; 45(4):538-44; J Cardiovasc Pharmacol. 2003 Jun; 41(6):955-63; Circulation. 2001 Jul 24; 104(4):467-72.
Chemical Name: methyl (4aS, 4bR, 5aR, 6aS, 7R, 9aS, 9bR, 10R)-4a, 6a-dimethyl-2, 5'-dioxo-2, 4, 4a, 4', 5a, 5', 6, 6a, 8, 9, 9a, 9b, 10, 11-tetradecahydro-3H, 3'H-spiro[cyclopenta[1, 2]phenanthro[4, 4a-b]oxirene-7, 2'-furan]-10-carboxylate
InChi Key: JUKPWJGBANNWMW-VWBFHTRKSA-N
InChi Code: InChI=1S/C24H30O6/c1-21-7-4-14(25)10-13(21)11-15(20(27)28-3)19-16-5-8-23(9-6-18(26)30-23)22(16, 2)12-17-24(19, 21)29-17/h10, 15-17, 19H, 4-9, 11-12H2, 1-3H3/t15-, 16+, 17-, 19+, 21+, 22+, 23-, 24-/m1/s1
SMILES Code: C[C]12CCC(C=C1C[CH](C(OC)=O)[CH]3[C]24[CH](C[C]5(C)[CH]3CC[C]56CCC(O6)=O)O4)=O
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