Table 2.
Nuclear Receptor | hPR | hAR | hGR |
---|---|---|---|
Radioligand | [3H] progesterone 0.5 nM | [3H] methyltrienolone 1 nM | [3H] dexamethasone 1.5 nM |
Inhibition (%) in the presence of 1 µM C-1 | 14.7% | −2.3% | 4.4% |
The binding inhibition rate (%) of compound C-1 for PR, AR, and GR was determined. Each recombinant human nuclear receptor was incubated with the indicated concentration of the radiolabeled ligand and 1 µM C-1 for 6–20 hr at 4 °C. Inhibitory effects of C-1 were determined by scintillation counting. These results show very low affinities of C-1 for other nuclear receptors. Abbreviation: AR, androgen receptor; GR, glucocorticoid receptor; PR, progesterone receptor.