Metabolism of [14C]-5-chloro-1,3-benzodioxol-4-amine in male Wistar-derived rats following intraperitoneal administration.
[14C]-5-chloro-1,3-benzodioxol-4-amine was administered intraperitoneally (i.p.) to bile duct-cannulated rats (Alpk:ApfSD, Wistar derived) at 25 mg kg-1 to determine the rates and routes of excretion of the compound and to investigate its metabolic fate. A total of 89.1% of the dose was excreted in the 48 h following administration, the majority being recovered in the urine during the first 12 h. The main metabolite in both urine and bile, detected by high-performance liquid chromatography (HPLC) with radioprofiling and mass spectrometry, was identified as a demethylenated monosulfate conjugate. Unchanged parent compound formed a major component of the radiolabel excreted in urine and, in addition to unchanged parent and demethylenated sulphate conjugate, a large number of minor metabolites were detected in urine and bile. The overall metabolic fate of 5-chloro-1,3-benzodioxol-4-amine in the rat was complex, with some similarities to previously studied methylenedioxyphenyl compounds.
Athersuch
T J
TJ
Department of Biomolecular Medicine, Division of Surgery, Oncology, Reproductive Biology and Anaesthetics (SORA), Faculty of Medicine, Imperial College London, London, UK.
Duckett
C J
CJ
Castro-Perez
J
J
Rodgers
C
C
Nicholson
J K
JK
Wilson
I D
ID
D000818:Animals; D052117:Benzodioxoles / Q000008:administration & dosage* / Q000378:metabolism / Q000493:pharmacokinetics* / Q000652:urine; D001646:Bile / Q000737:chemistry; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D008658:Inactivation, Metabolic; D007274:Injections, Intraperitoneal; D007536:Isomerism; D008297:Male; D013058:Mass Spectrometry; D051381:Rats; D017208:Rats, Wistar
C519623:5-chloro-1,3-benzodioxol-4-amine; D052117:Benzodioxoles; D002250:Carbon Radioisotopes