Metabolism of 2,3,5,6-tetrachloronitrobenzene (tecnazene) in rat

Lappin, Graham, Pritchard, D., Moore, R. B. and Laird, W. J. D. (1996) Metabolism of 2,3,5,6-tetrachloronitrobenzene (tecnazene) in rat. Xenobiotica, 26 (1). pp. 65-77. ISSN 0049-8254

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The metabolic fate of U- 14C-2,3,5,6-tetrachloronitrobenzene (tecnazene) has been determined in the male and female rat following a single dose of 1 mg/kg and in surgically prepared, bile-duct-cannulated rats following a single oral dose of 135 mg/kg. Radioactivity in the female rat was excreted mainly in urine (82%). The male rat, however, excreted approximately equal amounts of radioactivity in urine and faeces (the latter via bile). The principal metabolic pathway was conjugation with glutathione (GSH) and concomitant nitro-displacement. The GSH-conjugate and related metabolites were excreted in the bile and ultimately in the urine as the mercapturic acid conjugate. The cysteine conjugate underwent β-lyase-mediated metabolism to yield a thiol that underwent subsequent methylation to the thioanisole followed by S-oxidation. A novel tetrachloromethyldisulphide metabolite was also formed.

Keywords:2,3,5,6 tetrachloronitrobenzene, nitrobenzene derivative, unclassified drug, animal experiment, article, biliary excretion, conjugation, controlled study, feces, female, male, metabolite, methylation, nonhuman, oxidation, rat, sex difference, urinary excretion, xenobiotic metabolism, Animals, Biotransformation, Chromatography, High Pressure Liquid, Fungicides, Industrial, Gas Chromatography-Mass Spectrometry, Mass Spectrometry, Nitrobenzenes, Rats, Rats, Wistar, Tissue Distribution, Animalia
Divisions:College of Science > School of Pharmacy
ID Code:8247
Deposited On:21 Mar 2013 15:19

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