Template:Affinities of selected ligands at the androgen receptor

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Affinities of selected ligands at the androgen receptor

Compound AR RBA (%) AR Ki (nM)
Template:No selflink 100 1.18
Template:No selflink 136 0.87
Template:No selflink 117 1.01
Template:No selflink 67.0 1.76
Template:No selflink 14.8 8.0
Template:No selflink 13.6 8.7
Template:No selflink 12.5 9.5
Template:No selflink 6.6 18
Template:No selflink 4.9 24
Template:No selflink 2.0 58
Template:No selflink 0.84 140
Template:No selflink 0.079 1200
Template:No selflink 0.00084 140,000
Notes: (1) Human skin fibroblasts used for assays. (2) Situation in vivo is different for flutamide and spironolactone due biotransformation. (3) Conflicting findings for spironolactone. Sources: Main: [1][2] Related: [3][4][5]

References

  1. Hammerstein, J. (1990). "Antiandrogens: Clinical Aspects". Hair and Hair Diseases. pp. 827–886. doi:10.1007/978-3-642-74612-3_35. ISBN 978-3-642-74614-7.
  2. Eil C, Edelson SK (July 1984). "The use of human skin fibroblasts to obtain potency estimates of drug binding to androgen receptors". J. Clin. Endocrinol. Metab. 59 (1): 51–5. doi:10.1210/jcem-59-1-51. PMID 6725525.
  3. Brown TR, Rothwell SW, Sultan C, Migeon CJ (June 1981). "Inhibition of androgen binding in human foreskin fibroblasts by antiandrogens". Steroids. 37 (6): 635–48. doi:10.1016/S0039-128X(81)90173-2. PMID 6457421.
  4. Breiner M, Romalo G, Schweikert HU (August 1986). "Inhibition of androgen receptor binding by natural and synthetic steroids in cultured human genital skin fibroblasts". Klinische Wochenschrift. 64 (16): 732–7. doi:10.1007/BF01734339. PMID 3762019.
  5. Breiner M, Romalo G, Schweikert HU (1986). "Inhibition of androgen receptor binding by drugs in cultured human genital skin fibroblasts". Acta Endocrinologica. 113 (1_Suppl): S152. doi:10.1530/acta.0.111S152. ISSN 0804-4643.