TY  - JOUR
PY  - 1993//
TI  - Distribution of 1-aminobenzotriazole in male rats after administration of an oral dose
JO  - Xenobiotica
A1  - Town, C.
A1  - Henderson, L.
A1  - Chang, D.
A1  - Mortillo, M.
A1  - Garland, W.
SP  - 383
EP  - 390
VL  - 23
IS  - 4
N2  - 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.<p /> <p>Language: en</p>
LA  - en
SN  - 0049-8254
UR  - http://dx.doi.org/10.3109/00498259309057026
ID  - ref1
ER  -