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
^
abcdefBell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK (2007). "(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor". J. Med. Chem. 50 (26): 6443–5.
doi:
10.1021/jm701186z.
PMID18038968.
^
abcdeHasui 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.
PMID22074142.
^
abcdeHu 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.
PMID16101407.
^
abcdefghiYang 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.
PMID23777778.
^
abcdPitt 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.
PMID22562554.
^
abMeyers 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.
PMID20672822.
^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.
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
^
abcdefBell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK (2007). "(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor". J. Med. Chem. 50 (26): 6443–5.
doi:
10.1021/jm701186z.
PMID18038968.
^
abcdeHasui 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.
PMID22074142.
^
abcdeHu 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.
PMID16101407.
^
abcdefghiYang 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.
PMID23777778.
^
abcdPitt 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.
PMID22562554.
^
abMeyers 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.
PMID20672822.
^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.