Template:Spironolactone at steroid hormone receptors

v
t
e
Spironolactone at steroid hormone receptors
Site	Value (nM)	Type	Action	Species	Ref
ARTooltip Androgen receptor	39.4 120 13–670 >20,000	K_i IC₅₀^a IC₅₀^b EC₅₀	Antagonist	Human	^[1] ^[2] ^[3]^[4] ^[4]
ERTooltip Estrogen receptor^c	>1,100 5,700	K_i IC₅₀^b	Antagonist	Human	^[1] ^[3]
ERαTooltip Estrogen receptor alpha	5,970–>20,000 >20,000	IC₅₀^b EC₅₀	Agonist	Human	^[5]^[4] ^[4]
ERβTooltip Estrogen receptor beta	4940–>20,000 3,300	IC₅₀^b EC₅₀	Inconsistent	Human	^[5]^[4] ^[4]
GRTooltip Glucocorticoid receptor	32.6 1,400 2,410–6,920 >20,000	K_i IC₅₀^a IC₅₀^b EC₅₀	Antagonist	Human	^[1] ^[2] ^[5]^[6] ^[4]
MRTooltip Mineralocorticoid receptor	2.32 49 2.4–60 17.7	K_i IC₅₀^a IC₅₀^b K_b	Antagonist	Human	^[1] ^[2] ^[3]^[2] ^[1]
PRTooltip Progesterone receptor^c	400 650 >25,000 740–2,619	K_i IC₅₀^a IC₅₀^b EC₅₀	Agonist	Human	^[1] ^[2] ^[3]^[6] ^[5]^[3]
PR-BTooltip Progesterone receptor B	4,000 >20,000	IC₅₀^b 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

^ ^a ^b ^c ^d ^e ^f Bell 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. PMID 18038968.
^ ^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 K_i 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.

[pmid18038968-1] ^ ^a ^b ^c ^d ^e ^f Bell 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. PMID 18038968.

[pmid22074142-2] 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.

[pmid16101407-3] 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.

[pmid23777778-4] ^ ^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.

[pmid22562554-5] 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.

[pmid20672822-6] 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.

[BindingDB-7] "The Binding Database (Binding DB)". University of California, San Diego and ChemAxon. Retrieved 21 December 2017.

[PDSP-8] Roth, BL; Driscol, J. "PDSP K_i 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.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]