Template:Relative affinities of first-generation nonsteroidal antiandrogens for the androgen receptor

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Relative affinities of first-generation nonsteroidal antiandrogens for the androgen receptor
Species IC50 (nM) RBA (ratio)
Bicalutamide 2-Hydroxyflutamide Nilutamide Bica / 2-OH-flu Bica / nilu Ref
Rat 190 700 ND 4.0 ND [1]
Rat ~400 ~900 ~900 2.3 2.3 [2]
Rat ND ND ND 3.3 ND [3]
Rata 3595 4565 18620 1.3 5.2 [4]
Human ~300 ~700 ~500 2.5 1.6 [5]
Human ~100 ~300 ND ~3.0 ND [6]
Humana 2490 2345 5300 1.0 2.1 [4]
Footnotes: a = Controversial data. Sources: [7][8]

References

  1. ↑ Furr BJ, Valcaccia B, Curry B, Woodburn JR, Chesterson G, Tucker H (June 1987). "ICI 176,334: a novel non-steroidal, peripherally selective antiandrogen". J. Endocrinol. 113 (3): R7–9. doi:10.1677/joe.0.113R007. PMID 3625091.
  2. ↑ Teutsch G, Goubet F, Battmann T, Bonfils A, Bouchoux F, Cerede E, Gofflo D, Gaillard-Kelly M, Philibert D (January 1994). "Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor". J. Steroid Biochem. Mol. Biol. 48 (1): 111–9. doi:10.1016/0960-0760(94)90257-7. PMID 8136296.
  3. ↑ Winneker RC, Wagner MM, Batzold FH (December 1989). "Studies on the mechanism of action of Win 49596: a steroidal androgen receptor antagonist". J. Steroid Biochem. 33 (6): 1133–8. doi:10.1016/0022-4731(89)90420-2. PMID 2615358.
  4. ↑ 4.0 4.1 Luo, S; Martel, C; LeBlanc, G; Candas, B; Singh, S M; Labrie, C; Simard, J; Belanger, A; Labrie, F (1996). "Relative potencies of Flutamide and Casodex: preclinical studies". Endocrine Related Cancer. 3 (3): 229–241. doi:10.1677/erc.0.0030229. ISSN 1351-0088.
  5. ↑ Ayub M, Levell MJ (August 1989). "The effect of ketoconazole related imidazole drugs and antiandrogens on [3H] R 1881 binding to the prostatic androgen receptor and [3H]5 alpha-dihydrotestosterone and [3H]cortisol binding to plasma proteins". J. Steroid Biochem. 33 (2): 251–5. doi:10.1016/0022-4731(89)90301-4. PMID 2788775.
  6. ↑ Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen receptor stabilization". Urology. 48 (1): 157–63. doi:10.1016/S0090-4295(96)00117-3. PMID 8693644.
  7. ↑ Kolvenbag GJ, Furr BJ, Blackledge GR (December 1998). "Receptor affinity and potency of non-steroidal antiandrogens: translation of preclinical findings into clinical activity". Prostate Cancer Prostatic Dis. 1 (6): 307–314. doi:10.1038/sj.pcan.4500262. PMID 12496872.
  8. ↑ Manfred Wirth; J. E. Altwein; B. Schmitz-Dräger; S. Kuptz (1998). Molecular Biology of Prostate Cancer. Walter de Gruyter. pp. 92–. ISBN 978-3-11-080727-1.
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