Template:Relative affinities of antiandrogens at steroid-hormone receptors

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Relative affinities (%) of antiandrogens at steroid-hormone receptors
Antiandrogen AR PR ER GR MR
Cyproterone acetate 8–10 60 <0.1 5 1
Chlormadinone acetate 5 175 <0.1 38 1
Megestrol acetate 5 152 <0.1 50 3
Spironolactone 7 0.4a <0.1 2a 182
Trimethyltrienolone 3.6 <1 <1 <1 <1
Inocoterone 0.8 <0.1 <0.1 <0.1 <0.1
Inocoterone acetate <0.1 <0.1 <0.1 <0.1 <0.1
Flutamide <0.1 <0.1 <0.1 <0.1 <0.1
Hydroxyflutamide 0.5–0.8 <0.1 <0.1 <0.1 <0.1
Nilutamide 0.5–0.8 <0.1 <0.1 <0.1 <0.1
Bicalutamide 1.8 <0.1 <0.1 <0.1 <0.1
Notes: (1): Reference ligands (100%) were testosterone for the AR, progesterone for the PR, estradiol for the ER, dexamethasone for the GR, and aldosterone for the MR. (2): Tissues were rat prostate (AR), rabbit uterus (PR), mouse uterus (ER), rat thymus (GR), and rat kidney (MR). (3): Incubation times (0°C) were 24 hours (AR, a), 2 hours (PR, ER), 4 hours (GR), and 1 hour (MR). (4): Assay methods were different for bicalutamide for receptors besides the AR. Sources: [1][2][3][4][5][6][7][8][9][10]

References

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