Template:Spironolactone at steroid hormone receptors
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| Site | Value (nM) | Type | Action | Species | Ref |
|---|---|---|---|---|---|
| AR | 39.4 120 13–670 >20,000 |
Ki IC50a IC50b EC50 |
Antagonist | Human | [1] [2] [3][4] [4] |
| ERc | >1,100 5,700 |
Ki IC50b |
Antagonist | Human | [1] [3] |
| ERα | 5,970–>20,000 >20,000 |
IC50b EC50 |
Agonist | Human | [5][4] [4] |
| ERβ | 4940–>20,000 3,300 |
IC50b EC50 |
Inconsistent | Human | [5][4] [4] |
| GR | 32.6 1,400 2,410–6,920 >20,000 |
Ki IC50a IC50b EC50 |
Antagonist | Human | [1] [2] [5][6] [4] |
| MR | 2.32 49 2.4–60 17.7 |
Ki IC50a IC50b Kb |
Antagonist | Human | [1] [2] [3][2] [1] |
| PRc | 400 650 >25,000 740–2,619 |
Ki IC50a IC50b EC50 |
Agonist | Human | [1] [2] [3][6] [5][3] |
| PR-B | 4,000 >20,000 |
IC50b EC50 |
Antagonist | Human | [4] [4] |
| Notes: The ranges are the values reported in different studies. Footnotes: a = Binding inhibition. b = Functional antagonism. c = Subtype unspecified (probably ERα and PR-B, however). Sources: [7][8] | |||||
References
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- ^ a b c d e Hasui T, Matsunaga N, Ora T, Ohyabu N, Nishigaki N, Imura Y, Igata Y, Matsui H, Motoyaji T, Tanaka T, Habuka N, Sogabe S, Ono M, Siedem CS, Tang TP, Gauthier C, De Meese LA, Boyd SA, Fukumoto S (2011). "Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists". J. Med. Chem. 54 (24): 8616–31. doi:10.1021/jm2011645. PMID 22074142.
- ^ a b c d e Hu X, Li S, McMahon EG, Lala DS, Rudolph AE (2005). "Molecular mechanisms of mineralocorticoid receptor antagonism by eplerenone". Mini Rev Med Chem. 5 (8): 709–18. doi:10.2174/1389557054553811. PMID 16101407.
- ^ a b c d e f g h i Yang C, Shen HC, Wu Z, Chu HD, Cox JM, Balsells J, Crespo A, Brown P, Zamlynny B, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Bateman T, Xu L, Tong X, Crook M, Sinclair P (2013). "Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists". Bioorg. Med. Chem. Lett. 23 (15): 4388–92. doi:10.1016/j.bmcl.2013.05.077. PMID 23777778.
- ^ a b c d Pitt B, Filippatos G, Gheorghiade M, Kober L, Krum H, Ponikowski P, Nowack C, Kolkhof P, Kim SY, Zannad F (June 2012). "Rationale and design of ARTS: a randomized, double-blind study of BAY 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease". Eur. J. Heart Fail. 14 (6): 668–75. doi:10.1093/eurjhf/hfs061. PMID 22562554.
- ^ a b Meyers MJ, Arhancet GB, Hockerman SL, Chen X, Long SA, Mahoney MW, Rico JR, Garland DJ, Blinn JR, Collins JT, Yang S, Huang HC, McGee KF, Wendling JM, Dietz JD, Payne MA, Homer BL, Heron MI, Reitz DB, Hu X (2010). "Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy". J. Med. Chem. 53 (16): 5979–6002. doi:10.1021/jm100505n. PMID 20672822.
- ^ "The Binding Database (Binding DB)". University of California, San Diego and ChemAxon. Retrieved 21 December 2017.
- ^ Roth, BL; Driscol, J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.