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
- ↑ Verhoeven CH, Vos RM, Delbressine LP (2002). "The in vivo metabolism of tibolone in animal species". Eur J Drug Metab Pharmacokinet. 27 (1): 1–10. doi:10.1007/BF03190399. PMID 11996321.
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