Metabolism of the aromatase inhibitor 4-hydroxyandrostenedione in vivo. Identification of the glucuronide as a major urinary metabolite in patients and biliary metabolite in the rat.
4-Hydroxyandrost-4-ene-3,17-dione (HAD) is a potent and selective inhibitor of the enzyme complex aromatase, both in vitro and in vivo. The glucuronide is a major metabolite in the urine of patients and in the bile of rats given HAD and it was identified by chemical ionization-MS of the permethylated derivative. HAD glucuronide was quantified by first converting it enzymically into HAD, then determining HAD by capillary column GC-MS of the perfluorotolyl derivative using 4-hydroxyandrost-2,4-diene-3,17-dione as internal standard.
D000735:Androstenedione / Q000031:analogs & derivatives* / Q000378:metabolism / Q000652:urine; D000818:Animals; D047072:Aromatase Inhibitors; D001646:Bile / Q000378:metabolism*; D005260:Female; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D008099:Liver / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains
D047072:Aromatase Inhibitors; C048728:4-hydroxy-4-androstene-3,17-dione glucuronide; D000735:Androstenedione; C014594:formestane