Aromatization in vivo of 3 β, 17β-bisacetoxy-17α-ethynyl-19-nor-androst-4-ene (SC-II 800)

Abstract

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 μCi/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.