Template:Relative_affinities_of_noretynodrel,_tibolone,_and_metabolites
Template:Relative affinities of noretynodrel, tibolone, and metabolites
More information Compound, Code name ...
Compound | Code name | PRTooltip Progesterone receptor | ARTooltip Androgen receptor | ERTooltip Estrogen receptor | GRTooltip Glucocorticoid receptor | MRTooltip Mineralocorticoid receptor | SHBGTooltip Sex hormone-binding globulin | CBGTooltip Corticosteroid binding globulin |
---|---|---|---|---|---|---|---|---|
Noretynodrel | – | 6 | 0 | 2 | 0 | 0 | 0 | 0 |
Norethisterone (δ4-NYD) | – | 67–75 | 15 | 0 | 0–1 | 0–3 | 16 | 0 |
3α-Hydroxynoretynodrel | – | ? | ? | ? | ? | ? | ? | ? |
3β-Hydroxynoretynodrel | – | ? | ? | ? | ? | ? | ? | ? |
Ethinylestradiol | – | 15–25 | 1–3 | 112 | 1–3 | <1 | 0.18 | <0.1 |
Tibolone (7α-Me-NYD) | ORG-OD-14 | 6 | 6 | 1 | ? | ? | ? | ? |
Δ4-Tibolone | ORG-OM-38 | 90 | 35 | 1 | 0 | 2 | 1 | 0 |
3α-Hydroxytibolone | ORG-4094 | 0 | 3 | 4–6 | 0 | ? | ? | ? |
3β-Hydroxytibolone | ORG-301260 | 0 | 4 | 3–29 | 0 | ? | ? | ? |
7α-Methylethinylestradiol | – | ? | ? | ? | ? | ? | ? | ? |
Notes: Values are percentages (%). Reference ligands (100%) were promegestone for the PRTooltip progesterone receptor, metribolone for the ARTooltip androgen receptor, E2 for the ERTooltip estrogen receptor, DEXATooltip dexamethasone for the GRTooltip glucocorticoid receptor, aldosterone for the MRTooltip mineralocorticoid receptor, DHTTooltip dihydrotestosterone for SHBGTooltip sex hormone-binding globulin, and cortisol for CBGTooltip Corticosteroid-binding globulin. Sources: [1][2][3][4][5][6] |
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References
- Kuhl H (September 1990). "Pharmacokinetics of oestrogens and progestogens". Maturitas. 12 (3): 171–97. doi:10.1016/0378-5122(90)90003-O. PMID 2170822.
- Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947.
- Philibert D, Bouchoux F, Degryse M, Lecaque D, Petit F, Gaillard M (October 1999). "The pharmacological profile of a novel norpregnance progestin (trimegestone)". Gynecol. Endocrinol. 13 (5): 316–26. doi:10.3109/09513599909167574. PMID 10599548.
- Raynaud, J.P.; Ojasoo, T.; Bouton, M.M.; Philibert, D. (1979). "Receptor Binding as a Tool in the Development of New Bioactive Steroids". Drug Design: Medicinal Chemistry: A Series of Monographs. Vol. 8. pp. 169–214. doi:10.1016/B978-0-12-060308-4.50010-X. ISBN 978-0120603084.
- Pugeat MM, Dunn JF, Nisula BC (July 1981). "Transport of steroid hormones: interaction of 70 drugs with testosterone-binding globulin and corticosteroid-binding globulin in human plasma". J. Clin. Endocrinol. Metab. 53 (1): 69–75. doi:10.1210/jcem-53-1-69. PMID 7195405.
- Schoonen WG, Deckers GH, de Gooijer ME, de Ries R, Kloosterboer HJ (2000). "Hormonal properties of norethisterone, 7α-methyl-norethisterone and their derivatives". J. Steroid Biochem. Mol. Biol. 74 (4): 213–22. doi:10.1016/s0960-0760(00)00125-4. PMID 11162927.
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