7α-Methylestradiol explained
7α-Methylestradiol (7α-Me-E2), also known as 7α-methylestra-1,3,5(10)-triene-3,17β-diol, is a synthetic estrogen and an active metabolite of the androgen/anabolic steroids trestolone/Methandienone.[1] [2] [3] It is considered to be responsible for the estrogenic activity of trestolone. The compound shows about higher affinity for the estrogen receptor than estradiol.
Relative affinities (%) of 7α-methylestradiol and related steroids[4] [5] [6] | Compound | | | | | | | |
|---|
| 2.6 | 7.9 | 100 | 0.6 | 0.13 | 8.7 | <0.1 |
| 7α-Methylestradiol | 1–3 | 15–25 | 101 | <1 | <1 | ? | ? |
| 50–75 | 100–125 | ? | <1 | ? | ? | ? |
| Values are percentages (%). Reference ligands (100%) were progesterone for the, testosterone for the, for the, for the, aldosterone for the, for, and cortisol for . | |
See also
Notes and References
- Book: Raynaud JP, Ojasoo T, Bouton MM, Philibert D . Drug Design. Receptor Binding as a Tool in the Development of New Bioactive Steroids. 1979. 169–214. 10.1016/B978-0-12-060308-4.50010-X. 9780120603084. https://books.google.com/books?id=bhAlBQAAQBAJ&pg=PA169.
- García-Becerra R, Ordaz-Rosado D, Noé G, Chávez B, Cooney AJ, Larrea F . Comparison of 7α-methyl-19-nortestosterone effectiveness alone or combined with progestins on androgen receptor mediated-transactivation . Reproduction . 143 . 2 . 211–219 . February 2012 . 22065861 . 10.1530/REP-11-0171 . free .
- Attardi BJ, Pham TC, Radler LC, Burgenson J, Hild SA, Reel JR . Dimethandrolone (7alpha,11beta-dimethyl-19-nortestosterone) and 11beta-methyl-19-nortestosterone are not converted to aromatic A-ring products in the presence of recombinant human aromatase . The Journal of Steroid Biochemistry and Molecular Biology . 110 . 3–5 . 214–222 . June 2008 . 18555683 . 2575079 . 10.1016/j.jsbmb.2007.11.009 .
- Ojasoo T, Delettré J, Mornon JP, Turpin-VanDycke C, Raynaud JP . Towards the mapping of the progesterone and androgen receptors . Journal of Steroid Biochemistry . 27 . 1–3 . 255–269 . 1987 . 3695484 . 10.1016/0022-4731(87)90317-7 .
- Ojasoo T, Raynaud JP . Unique steroid congeners for receptor studies . Cancer Research . 38 . 11 Pt 2 . 4186–4198 . November 1978 . 359134 .
- Raynaud JP, Bouton MM, Moguilewsky M, Ojasoo T, Philibert D, Beck G, Labrie F, Mornon JP . 6 . Steroid hormone receptors and pharmacology . Journal of Steroid Biochemistry . 12 . 143–157 . January 1980 . 7421203 . 10.1016/0022-4731(80)90264-2 .
