Metabolic disposition of chlorambucil in rats.
1. The metabolic dispositionof chlorambucil, 4-p-(di-2-chloroethyl)aminophenylbutyric acid, was studied in the rat. 2. After oral administration of [14C]chlorambucil to rats, plasma, liver, and kidney showed the highest concentration of 14C. After intravenous administration, plasma and kidney were heavily labelled. Although plasma contained as much as 10% of the administered dose in the first few hours after administration, the level decreased to 1% by 24 h. Elimination of radioactivity was mainly through the kidney. 3. Ten metabolites were isolated and characterized by mass spectrometry. Most metabolites had undergone oxidation on the butyric acid side-chain to form phenylacetic acid and benzoic acid derivatives. Spontaneous degradation products of [14C]chlorambucil were analysed and compared with the metabolites.
D000284:Administration, Oral; D000818:Animals; D002699:Chlorambucil / Q000097:blood / Q000378:metabolism* / Q000652:urine; D002849:Chromatography, Gas; D004764:Enterohepatic Circulation; D007275:Injections, Intravenous; D007408:Intestinal Absorption; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D013058:Mass Spectrometry; D051381:Rats; D013997:Time Factors
D002699:Chlorambucil