Template:Selected biological properties of endogenous estrogens in rats
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| Estrogen | ER RBA (%) | Uterine weight (%) | Uterotrophy | LH levels (%) | SHBG RBA (%) |
|---|---|---|---|---|---|
| Control | – | 100 | – | 100 | – |
| Estradiol | 100 | 506 ± 20 | +++ | 12–19 | 100 |
| Estrone | 11 ± 8 | 490 ± 22 | +++ | ? | 20 |
| Estriol | 10 ± 4 | 468 ± 30 | +++ | 8–18 | 3 |
| Estetrol | 0.5 ± 0.2 | ? | Inactive | ? | 1 |
| 17α-Estradiol | 4.2 ± 0.8 | ? | ? | ? | ? |
| 2-Hydroxyestradiol | 24 ± 7 | 285 ± 8 | +b | 31–61 | 28 |
| 2-Methoxyestradiol | 0.05 ± 0.04 | 101 | Inactive | ? | 130 |
| 4-Hydroxyestradiol | 45 ± 12 | ? | ? | ? | ? |
| 4-Methoxyestradiol | 1.3 ± 0.2 | 260 | ++ | ? | 9 |
| 4-Fluoroestradiola | 180 ± 43 | ? | +++ | ? | ? |
| 2-Hydroxyestrone | 1.9 ± 0.8 | 130 ± 9 | Inactive | 110–142 | 8 |
| 2-Methoxyestrone | 0.01 ± 0.00 | 103 ± 7 | Inactive | 95–100 | 120 |
| 4-Hydroxyestrone | 11 ± 4 | 351 | ++ | 21–50 | 35 |
| 4-Methoxyestrone | 0.13 ± 0.04 | 338 | ++ | 65–92 | 12 |
| 16α-Hydroxyestrone | 2.8 ± 1.0 | 552 ± 42 | +++ | 7–24 | <0.5 |
| 2-Hydroxyestriol | 0.9 ± 0.3 | 302 | +b | ? | ? |
| 2-Methoxyestriol | 0.01 ± 0.00 | ? | Inactive | ? | 4 |
| Notes: Values are mean ± SD or range. ER RBA = Relative binding affinity to estrogen receptors of rat uterine cytosol. Uterine weight = Percentage change in uterine wet weight of ovariectomized rats after 72 hours with continuous administration of 1 μg/hour via subcutaneously implanted osmotic pumps. LH levels = Luteinizing hormone levels relative to baseline of ovariectomized rats after 24 to 72 hours of continuous administration via subcutaneous implant. Footnotes: a = Synthetic (i.e., not endogenous). b = Atypical uterotrophic effect which plateaus within 48 hours (estradiol's uterotrophy continues linearly up to 72 hours). Sources: [1][2][3][4][5][6][7][8][9] | |||||
Template documentationSee also
- Estrogen (medication) § Pharmacology
- Template:Affinities of estrogen receptor ligands for the ERα and ERβ
- Template:Relative affinities of estrogens for steroid hormone receptors and blood proteins
References
- ↑ "Uterine estrogen receptor binding of catecholestrogens and of estetrol (1,3,5(10)-estratriene-3,15alpha,16alpha,17beta-tetrol)". Steroids 27 (3): 325–33. March 1976. doi:10.1016/0039-128x(76)90054-4. PMID 178074.
- ↑ "Direction of estradiol metabolism as a control of its hormonal action--uterotrophic activity of estradiol metabolites". Endocrinology 101 (6): 1709–15. December 1977. doi:10.1210/endo-101-6-1709. PMID 590186.
- ↑ "Differential biological activity of estradiol metabolites". Pediatrics 62 (6 Pt 2): 1128–33. December 1978. PMID 724350. https://pediatrics.aappublications.org/content/62/6/1128.
- ↑ "Impact of continuously administered catechol estrogens on uterine growth and luteinizing hormone secretion". Endocrinology 105 (6): 1288–92. December 1979. doi:10.1210/endo-105-6-1288. PMID 499073.
- ↑ Fishman, J.; Martucci, C. P. (1980). "New Concepts of Estrogenic Activity: the Role of Metabolites in the Expression of Hormone Action". The Menopause and Postmenopause. pp. 43–52. doi:10.1007/978-94-011-7230-1_5. ISBN 978-94-011-7232-5.
- ↑ "Biological properties of 16 alpha-hydroxyestrone: implications in estrogen physiology and pathophysiology". J. Clin. Endocrinol. Metab. 51 (3): 611–5. September 1980. doi:10.1210/jcem-51-3-611. PMID 7190977.
- ↑ "The role of 2-methoxyestrone in estrogen action". J. Steroid Biochem. 19 (1B): 635–8. July 1983. doi:10.1016/0022-4731(83)90229-7. PMID 6310247.
- ↑ John A. McLachlan, ed. "Dissociation of biological activities in metabolites of estradiol". Estrogens in the Environment: Proceedings of the Symposium on Estrogens in the Environment, Raleigh, North Carolina, U.S.A., September 10-12, 1979. Elsevier. pp. 131–145. ISBN 9780444003720. https://books.google.com/books?id=eu5qAAAAMAAJ.
- ↑ "Pharmacology of estrogens and progestogens: influence of different routes of administration". Climacteric 8 Suppl 1: 3–63. 2005. doi:10.1080/13697130500148875. PMID 16112947. http://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1313155660.pdf.
