Metabolism of 2-3H- and 4-14C-17alpha-ethynylestradiol 3-methyl ether (mestranol) by women.
A mixture of 2-3H and 4-14C-mestranol was administered orally to five women and 2-3H-mestranol alone to one woman. Reactions involving position 2 were extensive as judged by liberation of 3H into body water (14-45% of the dose). 17alpha-Ethynylestradiol, 2-hydroxy-17alpha-ethynylestradiol, 2-methoxy-17alpha-ethynylestradiol, 2-hydroxy-17alpha-ethynylestradiol 3-methyl ether and 16geta-hydroxy-17alpha-ethynylestradiol were measured in the "glucuronide" and pH1 fractions and mestranol, D-homoestrone-17a and D-homoestradiol-17abeta were also measured in the "glucuronide" fraction frum the urine to two of the women by reverse isotope dilution. Radioactive 2-methoxyestradiol accounted for less than 0.011% of the 14C dose in the "glucuronide" fraction of one of the women, consistent with the extent of de-ethynylation previously reported (Steroids, 25, 343 (1975).
D000328:Adult; D001827:Body Height; D001834:Body Water / Q000378:metabolism; D001835:Body Weight; D002250:Carbon Radioisotopes; D005260:Female; D005965:Glucuronates / Q000652:urine; D006801:Humans; D008656:Mestranol / Q000378:metabolism* / Q000494:pharmacology; D009640:Norethindrone / Q000494:pharmacology; D014316:Tritium
D002250:Carbon Radioisotopes; D005965:Glucuronates; D014316:Tritium; D008656:Mestranol; D009640:Norethindrone