Metabolism of [14C]-5-chloro-1,3-benzodioxol-4-amine in male Wistar-derived rats following intraperitoneal administration

ATHERSUCH, Toby, DUCKETT, Catherine, CASTRO-PEREZ, Jose, WILSON, Ian and NICHOLSON, Jeremy (2008). Metabolism of [14C]-5-chloro-1,3-benzodioxol-4-amine in male Wistar-derived rats following intraperitoneal administration. Xenobiotica, 37 (1), 44-58.

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[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.

Item Type: Article
Uncontrolled Keywords: Methylenedioxyphenyl, metabolism, high-performance liquid chromatography/mass spectrometry (HPLC-MS)
Research Institute, Centre or Group: Biomolecular Sciences Research Centre
Departments: Health and Well-being > Department of Bioscience
Identification Number:
Depositing User: Catherine Duckett
Date Deposited: 17 Jan 2018 14:46
Last Modified: 30 Apr 2019 11:53

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