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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1993-8-26
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pubmed:abstractText |
1. 14C-labelled 1-aminobenzotriazole (ABT), a suicide inactivator of cytochrome P450, was synthesized and administered orally to male rats. The rats were killed at 1, 6, 24, 48 or 72 h after dosing and the concentration of total radioactivity in various tissues and organs measured. 2. The compound appears to be absorbed slowly with 50% of the radioactivity remaining in the stomach at 6 h after dosing and maximum plasma and tissue concentrations were observed at 24 h. 3. Approximately 71% of the dose of 14C was excreted in the urine and 12% in the faeces over 72 h, indicating oral absorption of at least 71%. Tissue-to-plasma ratios of 14C were highest in the liver, adrenals and kidneys, which all contain significant amounts of cytochrome P450; the half-lives of elimination for total 14C in liver, adrenals and kidneys were approximately 24, 16 and 12 h, respectively, while the half-life in plasma was approximately 9 h. 4. ABT was metabolized by N-acetylation, with the acetylated product attaining concentrations equal to ABT in the plasma; two other major metabolites were also excreted in the urine namely, the N-glucuronide of 1-aminobenzotriazole and the N-glucuronide of benzotriazole.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0049-8254
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
383-90
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:8337896-Administration, Oral,
pubmed-meshheading:8337896-Animals,
pubmed-meshheading:8337896-Biotransformation,
pubmed-meshheading:8337896-Chromatography, High Pressure Liquid,
pubmed-meshheading:8337896-Half-Life,
pubmed-meshheading:8337896-Male,
pubmed-meshheading:8337896-Rats,
pubmed-meshheading:8337896-Tissue Distribution,
pubmed-meshheading:8337896-Triazoles
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pubmed:year |
1993
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pubmed:articleTitle |
Distribution of 1-aminobenzotriazole in male rats after administration of an oral dose.
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pubmed:affiliation |
Department of Drug Metabolism, Hoffmann-La Roche Inc., Nutley, NJ 07110.
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pubmed:publicationType |
Journal Article
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