Aromatization and hydrolysis of norethisterone-3-oxime in rabbit.
Two pharmacologically active metabolites, norethisterone (NET) and ethinylestradiol (EE2), were detected by HPLC and HPLC-RIA methods in rabbit plasma following single i.v. and i.g. administration at a dose of 1 mg/20 microCi/kg of [3H]norethisterone-3-oxime (NETO). Approximately 48% (i.v. injection) and 91% (i.g. administration) of the NETO dose were hydrolyzed to NET. Although only 0.35% of the NETO dose was aromatized to EE2, due to its high estrogenic potency, EE2 might contribute to the overall pharmacological pattern of NETO in the rabbit.
Department of Pharmacology, Walter Reed Army Institute of Research, Washington, DC 20307-5100.
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D000818:Animals; D001141:Aromatase / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004997:Ethinyl Estradiol / Q000097:blood; D005260:Female; D006868:Hydrolysis; D009640:Norethindrone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D011355:Prodrugs / Q000493:pharmacokinetics; D011817:Rabbits; D011863:Radioimmunoassay
D011355:Prodrugs; C016623:norethisterone-3-oxime; D004997:Ethinyl Estradiol; D001141:Aromatase; D009640:Norethindrone