Английская Википедия:Estradiol 3-saccharinylmethyl ether
Шаблон:Short description Шаблон:Drugbox
Estradiol 3-saccharinylmethyl ether (E2SME), also known as 3-O-(saccharinylmethyl)-17β-estradiol, is a synthetic estrogen and estrogen ether – specifically, the C3 saccharinylmethyl ether of estradiol – which was described in the mid-1990s and was never marketed.[1][2][3][4] It is a prodrug of estradiol and appears to be partially protected from first-pass metabolism in the liver and intestines with oral administration, showing greatly improved oral potency compared to estradiol.[2][3][4]
E2SME has been found to be 9-fold as potent as estradiol by the oral route in rats.[2][4] Similarly, its bioavailability (16%) was 5-fold greater than that of estradiol via the oral route in rats, and the elimination half-life of released estradiol was 5- to 7-fold longer than that of regular estradiol.[2][3][4] Conversely, when E2SME and estradiol were given intravenously in rats, there was no difference between them in terms of potency.[2] In vitro studies revealed that E2SME is not hydrolyzed to estradiol enzymatically but rather is hydrolyzed chemically in biological media such as plasma, apparently dependent on the concentration of protein.[2]
See also
References
Шаблон:Estrogen receptor modulators
Шаблон:Steroid-stub Шаблон:Genito-urinary-drug-stub
