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.
Li
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Department of Pharmacology, Walter Reed Army Institute of Research, Washington, DC 20307-5100.
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