17-p-estradiol

The influence of gonadal hormones on prepubertal animals suggests some steroidal sensitivity in adults with regard to F. elicitation. Young male sheep are induced to perform F. in response to exogenous T and to 17-p-estradiol F. in female red deer is also sensitive to T injections (Parrott, 1978 Fletcher, 1978). Sex differences can interact with the hormonal state where social conditions vary. Female cats (intact) display F. to urine marks only in the absence of males testosterone propionate induced F. in spayed females towards estrous females (Verbeme, 1976 Hart and Leedy, 1987), whereas an ovarian hormone (estradiol) failed to elicit F. to males (intact, and sexually inactive), presumably indicative of social inhibition overriding steroid facilitation. 

Le Bras, J. Rager, M. N. Besace, Y. Vaissermann, J. Amouri, H. Activation and regioselective ortho-functionalization of the A-ring of P-estradiol promoted by Cplr an efficient organometallic procedure for the synthesis of 2-methoxyestradiol. Organometallics 1997, 16, 1765-1771. 

To reduce conjugative first-pass metabolism and increase the oral bioavailability of P-estradiol, estradiol-3-salicylate, and P-estradiol-3-anthranilate, ester prodrugs were synthesized and their oral bioavailabilities in dogs were evaluated... 

With these promoieties, the 3-phenolic hydroxy group of p-estradiol (the normally metabolized functional group) was blocked so that first-pass conjugative metabolism could be reduced. The relative bioavailability of estradiol was significantly improved when administered in these prodrug forms. A 17-fold increase was observed with the estradiol-3-salicylate. The P-estradiol-3-anthrani-late increased the systemic availability five-fold. 

In a similar type of data collection, during 2000 to 2001 Wozniak (2002) examined the incidence of anabolic hormone residues in 5393 animals, consisting of cattle, pigs, horses, rabbits, chickens, geese, turkeys, ducks, and fish. Wozniak assayed for residues of diethylstibestrol, hexesterol, dienestrol, zeranol, trenbolone, and 19-noresterone. In addition, 632 cattle and swine were assayed for medroxyprogesterone and 1176 were assayed for natural 17-p-estradiol and testosterone. In only three heifers and two cows did serum testosterone exceed the MRL (EC 0.5 pg per liter) two bulls and four cows had an increased content of 17-(3-estradiol in their blood. A total of 11 animals of the 5393 examined (0.2%) had excessive quantities of hormone materials in their system. None of the other animals showed evidence of the presence of... 

Human prolactin is similar in structure to human growth hormone, and both are good lactogens. In women, prolactin acts with other hormones on the mammary gland during pregnancy to develop lactation and after birth to maintain it. Hyperprolactinemia causes impotence in men and amenorrhea and infertility in women. Chronically elevated levels of circulating prolactin are associated with suppression of 17-p-estradiol and testosterone production in the ovaries and testes. 

Arterial endothelial injury. Environmental smoke, administered to ovariectomized rats treated with subcutaneous placebo or 17 p-estradiol pellets for 6 weeks, produced a more than fourfold increase of carotid artery low-density lipoprotein (LDL) accumulation compared with filtered air exposure. The effect was largely mediated by increased permeability. No protective effect of estradiol was observed. Acute smoke exposure of a buffer solution containing LDL produced a more than sixfold increase in the highly reactive carbonyl glyoxal. Perfusion of this solution through carotid arteries produced 105% increase in permeability. Perfusion of glyoxal alone produced a 50% increase in carotid artery permeability ... 

P450 IA2 -fin women Inhibited by P-estradiol, progesterone, and OCs Caffeine, theophylline, demethylation of TCAs Fluvoxamine... 

The primary estrogen in premenopausal women is 17-P-estradiol (E2), which is synthesized by developing ovarian follicles. Estradiol is oxidized to estrone (El) and then to estriol (E3). Estrone is also produced in peripheral tissues... 

As noted above, 17-P-estradiol has hardly been used by the oral route, except in micronized form. The micronized product is also available in the form of an intranasal spray for the treatment of menopausal symptoms this can give rise to mild irritation, leading to sneezing (1). 

The minimum dose of continuously administered nor-ethindrone acetate needed to reduce significantly the incidence of endometrial hyperplasia associated with the use of 17-P-estradiol 1 mg/day has been investigated in a large, controlled, comparative study in 1146 women over 12 months (107). The results suggested that continuous norethindrone acetate at doses as low as 0.1 mg/day is fully effective, at least during the first year of treatment. 

Intranasal estradiol gives results comparable to transdermal estradiol, but substantially higher doses are needed. In 300 postmenopausal women, 17-P-estradiol 300 micro-grams/day was as effective as two patches per week delivering 50 micrograms/day (220). Adverse events rates were similar but moderate, and severe mastalgia was significantly less frequent with intranasal estradiol (7.2%) than with the patch (15.5%) 66% of the patients chose to continue the intranasal therapy and 34% the transdermal therapy. 

Allergic contact dermatitis from transdermal estrogen has been described in Korea, where the reaction was found to be due to 17-P-estradiol itself and not to an excipient (226). In some cases, allergic reactions and systemic contact dermatitis are clearly attributable to the patch material or to excipients. Even natural estradiol given in this way can occasionally cause hypersensitivity reactions, as determined by patch tests (227). 

Liu, R, Higuchi, W., Ghanem, A., Bergstrom, T., and Good, W. Assessing the influence of ethanol on simultaneous diffusion and metabolism of P-estradiol in hairless mouse skin for the asymmetric situation in vitro. Int. J. Pharm. 78 123-136, 1992. 

Suzuki K, Hirai H, Murata H et al (2003) Removal of estrogenic activities of 17[P]-estradiol and ethinylestradiol by ligninolytic enzymes from white rot fungi. Water Res 37 1972-1975... 

Pharmacodynamics Serum progesterone and 17-P-estradiol levels are considered reliable indicators for the occurrence of ovulation. Since progesterone and 17-f)-cstradiol levels were comparable for both treatments, and progesterone serum concentrations did not exceed 1.4 ng/mL (as defined in this study, progesterone concentrations above 1.4 ng/mL on day 20 of a menstrual cycle indicated ovulation) for both treatments, it was concluded that Drug XYZ administration did not affect the contraceptive effect of ethinylestradiol-based oral contraceptives and that no ovulation occurred in any of the subjects. 

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