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Estradiol is an estrogen, or an agonist of the nuclear estrogen receptors (ERs), the estrogen receptor alpha (ERα) and the estrogen receptor beta (ERβ). [1] [2] [6] In one study, the EC 50 Tooltip half-maximal effective concentration value of estradiol for the human ERα was 50 pM (0.05 nM) and for the human ERβ was 200 pM (0.2 nM).
Estrogen levels after a single dose of estradiol by different routes ; Route Dose (mg) Time measured ΔE2 levels (pg/mL) ΔE1 levels (pg/mL) E2:E1 ratio Ref Oral 1 2 4: 12 h 3 h 6 h +25 +40 ...
In the normal menstrual cycle, estradiol levels measure typically <50 pg/mL at menstruation, rise with follicular development (peak: 200 pg/mL), drop briefly at ovulation, and rise again during the luteal phase for a second peak. At the end of the luteal phase, estradiol levels drop to their menstrual levels unless there is a pregnancy.
Estradiol (E2) is a medication and naturally occurring steroid hormone. [11] [12] [13] It is an estrogen and is used mainly in menopausal hormone therapy and to treat low sex hormone levels in women.
[91] [96] [97] One study found that estrone sulfate levels were 200-fold higher than estradiol levels with 2 mg/day oral micronized estradiol or oral estradiol valerate, and estrone sulfate levels can reach up to nearly 1,000-fold higher concentrations than estradiol in some cases.
Quantitatively, estrogens circulate at lower levels than androgens in both men and women. [6] While estrogen levels are significantly lower in males than in females, estrogens nevertheless have important physiological roles in males. [7] Like all steroid hormones, estrogens readily diffuse across the cell membrane.
The influence of 2 mg/day oral estradiol valerate on coagulation factors is less than that of 10 μg/day oral ethinylestradiol. [93] [26] [94] [95] [96] Oral ethinylestradiol at 10 μg/day has been found to have about 1.5- to 2.5-fold the impact of 2 mg/day oral estradiol valerate on HDL cholesterol and triglycerides.
Polyestradiol phosphate (PEP), sold under the brand name Estradurin, is an estrogen medication which is used primarily in the treatment of prostate cancer in men. [1] [9] [2] [10] It is also used in women to treat breast cancer, as a component of hormone therapy to treat low estrogen levels and menopausal symptoms, and as a component of feminizing hormone therapy for transgender women.