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Metabolism and excretion of a new 5-lipoxygenase inhibitor in rats, Guinea-pigs, beagles and rhesus monkeys

Xenobiotica, ISSN: 0049-8254, Vol: 21, Issue: 5, Page: 627-634
1991
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1. The 5-lipoxygenase inhibitor (I), a substituted benzothiazole, is metabolized mainly by glucuronide and/or sulphate conjugation in rat, guinea-pig, beagle and rhesus monkey. Glucuronidation is the major pathway, and sulphation is more extensive in rat and beagle than in guinea-pig and rhesus monkey. 2. After a single oral dosing of C-I (10mg/kg), more than 96% of the dose was excreted in 7 days in all four species, however there is species difference in urinary excretion, which was 2.8 + 0.3% in rat, 46.9.1.6% in guinea-pig, 2.6% in beagle and 68.2% in rhesus monkey. 3. After a single i.v. dose of C-I to bile duct-cannulated rats and guinea pigs, bile was a major route of elimination, and in rats the ratio of glucuronide to sulphate in excreta increased from 0.71.0.01 to 0.93.0.05 as the dose was increased from 0.2 to 20mg/kg. © 1991 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.

Bibliographic Details

T. Yoshimura; S. Tanaka; H. Sakurai; Y. Nagai; K. Yamada; S. Katayama; S. Abe; I. Yamatsu

Informa UK Limited

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Environmental Science

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