| Compound | Synonym | Proportion (%) | Relative potency in the vagina (%) |
Relative potency in the uterus (%) |
RBA for ERα (%) |
RBA for ERβ (%) |
ERα / ERβ RBA ratio |
|---|---|---|---|---|---|---|---|
| Conjugated estrogens | – | 100 | 38 | 100 | – | – | – |
| Estrone | – | 49.1–61.5 | 30 | 32 | 26 | 52 | 0.50 |
| Equilin | Δ7-Estrone | 22.4–30.5 | 42 | 80 | 13 | 49 | 0.26 |
| 17α-Dihydroequilin | Δ7-17α-Estradiol | 13.5–19.5 | 0.06 | 2.6 | 41 | 32 | 1.30 |
| 17α-Estradiol | – | 2.5–9.5 | 0.11 | 3.5 | 19 | 42 | 0.45 |
| Δ8-Estrone | – | 3.5–3.9 | ? | ? | 19 | 32 | 0.60 |
| Equilenin | Δ6,8-Estrone | 2.2–2.8 | 1.3 | 11.4 | 15 | 20–29 | 0.50–0.75 |
| 17β-Dihydroequilin | Δ7-17β-Estradiol | 0.5–4.0 | 83 | 200 | 113 | 108 | 1.05 |
| 17α-Dihydroequilenin | Δ6,8-17α-Estradiol | 1.2–1.6 | 0.018 | 1.3 | 20 | 49 | 0.40 |
| 17β-Estradiol | – | 0.56–0.9 | 100 | ? | 100 | 100 | 1.00 |
| 17β-Dihydroequilenin | Δ6,8-17β-Estradiol | 0.5–0.7 | 0.21 | 9.4 | 68 | 90 | 0.75 |
| Δ8-17β-Estradiol | – | Small amounts | ? | ? | 68 | 72 | 0.94 |
| Notes: All listed compounds are present in conjugated estrogen products specifically in the form of the sodium salts of the sulfate esters (i.e., as sodium estrone sulfate, sodium equilin sulfate, etc.).[1][2] Sources: [1][3][2][4][5] | |||||||
References
edit- ^ a b 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.
- ^ a b Marc A. Fritz; Leon Speroff (28 March 2012). Clinical Gynecologic Endocrinology and Infertility. Lippincott Williams & Wilkins. pp. 751–. ISBN 978-1-4511-4847-3.
- ^ Bhavnani BR, Stanczyk FZ (July 2014). "Pharmacology of conjugated equine estrogens: efficacy, safety and mechanism of action". J. Steroid Biochem. Mol. Biol. 142: 16–29. doi:10.1016/j.jsbmb.2013.10.011. PMID 24176763.
- ^ Sweetman, Sean C., ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. p. 2087. ISBN 978-0-85369-840-1.
- ^ Bhavnani BR, Tam SP, Lu X (October 2008). "Structure activity relationships and differential interactions and functional activity of various equine estrogens mediated via estrogen receptors (ERs) ERalpha and ERbeta". Endocrinology. 149 (10): 4857–70. doi:10.1210/en.2008-0304. PMID 18599548.