Template:Absolute activities of tibolone and metabolites
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| Compound | Code name | PR | AR | ERα | ERβ | GR | MR |
|---|---|---|---|---|---|---|---|
| Template:No selflink | ORG-OD-14 | 123 | 1.05 | 4 | 105 | 2410* | 170* |
| Template:No selflink | ORG-OM-38 | 46 | 0.2 | 26 | 300 | 1760* | 30* |
| Template:No selflink | ORG-4094 | 2400* | 135* | 1.7 | 100 | ND* | 1160* |
| Template:No selflink | ORG-30126 | 20000* | ND* | 2.4 | 115 | ND* | 3310* |
| Notes: Values are affinities (nM). Non-italicized values are EC50. Italicized values with an asterisk (*) are IC50. Reference ligands (EC50) were promegestone (5 nM for PR), metribolone (0.1 nM for AR), estradiol (0.018 nM for ERα, 0.08 nM for ERβ), dexamethasone (6 nM for GR), and aldosterone (0.36 nM for MR). Sources: [1] | |||||||
References
- ↑ Escande A, Servant N, Rabenoelina F, Auzou G, Kloosterboer H, Cavaillès V, Balaguer P, Maudelonde T (August 2009). "Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites". J. Steroid Biochem. Mol. Biol. 116 (1–2): 8–14. doi:10.1016/j.jsbmb.2009.03.008. PMID 19464167.
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