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Recent basic and clinical advances have consolidated the concept of tissue-selective estrogens, i. It is metabolized in the human in at least a ratio to its 17beta form, 17beta-delta8,9-DHES. Hot women Paulista evaluate its activity in different clinical and biochemical parameters, a clinical research study was conducted with delta8,9-DHES and estrone sulfate as a comparator in postmenopausal women. Delta8,9-DHES was given orally at a daily dose of 0. Two additional groups of women received either estrone sulfate alone 1. This level of activity was equal to that obtained with the much higher dose of estrone sulfate, and it was sustained for the duration of the treatment period 12 weeks.
Measurements of a bone resorption marker, i. Gonadotropin secretion FSH and LH was ificantly suppressed in women receiving delta8,9-DHES, similar to that observed with estrone sulfate alone or with the combination of the two. Other parameters, such as total cholesterol, low density lipoprotein cholesterol and high density lipoprotein cholesterol were not modified ificantly, whereas serum globulins sex hormone-binding globulin and corticosteroid-binding globulin showed only marginal increases after delta8,9-DHES administration. Taken together with preclinical data, it is found that delta8,9-DHES is an active estrogen with a distinct pharmacological profile that in ificant clinical activity in vasomotor, neuroendocrine gonadotropin and PRL and bone preservation parameters, whereas displaying little or no efficacy, at the dose tested, on other peripheral parameters normally affected by estrogens.
Collectively, this information supports the concept that delta8,9-DHES is an integral component of CEE, with distinct tissue selectivity contributing to the CEE's overall clinical activity, and places this estrogen as a distinct member of a novel class of centrally active molecules with unique peripheral tissue selectivity. Please enable it to take advantage of the complete set of features!
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Similar articles Pharmacokinetics and pharmacodynamics of a novel estrogen delta8-estrone in postmenopausal women and men. Bhavnani BR, et al. J Steroid Biochem Mol Biol. PMID: Biologic effects of deltaestrone sulfate in postmenopausal women. J Soc Gynecol Investig. Differential effects of estrogen-androgen and estrogen-only therapy on vasomotor symptoms, gonadotropin secretion, and endogenous androgen bioavailability in postmenopausal women.
Simon J, et al. Tissue-selective estrogen complexes for postmenopausal women.
Mirkin S, Komm BS. Mirkin S, et al. Epub Jul PMID: Review. Pharmacokinetics and pharmacodynamics of conjugated equine estrogens: chemistry and metabolism. Bhavnani BR. Proc Soc Exp Biol Med. See all similar articles. Talboom JS, et al.
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MeSH terms Adult Actions. Female Actions. Humans Actions. Middle Aged Actions. Pilot Projects Actions. Substances 8,9-dehydroestrone sulfate Actions. Estrogens Actions. Estrone Actions. Full text links [x] Silverchair Information Systems. Copy Download.Hot women Paulista
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