RT Journal Article
SR Electronic
T1 The metabolism of mianserin in women, rabbits, and rats: identification of the major urinary metabolites.
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 48
OP 53
VO 9
IS 1
A1 G D de Jongh
A1 H M van den Wildenberg
A1 H Nieuwenhuyse
A1 F van der Veen
YR 1981
UL http://dmd.aspetjournals.org/content/9/1/48.abstract
AB The biotransformation of orally administered 3H-mianserin was investigated in female human subjects, rabbits, and rats by identification of the major urinary metabolites. Three days after dosing, the urinary excretion of radioactivity was 53% in women, 36% in rats, and 80% in rabbits. In the women's urine, 15% of the administered dose was excreted in the form of mianserin (conjugated plus nonconjugated); in the animal species this quantity was 1-2%. Mianserin was predominantly metabolized to 8-hydroxy analogs in all species; in rats, 8-hydroxydesmethylmianserin was the principal metabolite. Demethylation was an important metabolic pathway in the animal species, but not in women. Novel N-formyl compounds were detected in the urine of both animal species, but the possibility that these were artifacts formed during extraction with chloroform cannot be ruled out. Trace amounts of two compounds in which the piperazine moiety of mianserin was absent, 11H-dibenz[b,e]azepine and 11 H-dibenz[b,e]azepine-2-ol, were identified in the urine of rabbits and rats, respectively.