PMID: 7090416Jan 1, 1982Paper

Species differences in the disposition and metabolism of 1-methyl-3-(3-pyridyl)-5-(2-hydroxy-methylphenyl)-1H-1,2,4-triazole, a potential sedative-hypnotic compound

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
A AssandriE Martinelli


1. Disposition and metabolism of 1-methyl-3-(3-pyridyl)-5-(2-hydroxy-methylphenyl)-1H-1,2,4-triazole, a new sedative-hypnotic, were studied in rats (i.v. and p.o.), cats (i.v.) and human volunteers (p.o.) with 14C-labelled drug. 2. In rat and man, the compound is well absorbed, extensively metabolized, and excreted mostly through the kidney; it has short plasma half-lives, 0.6 h in rat, 0.9 h in man, and 1.9 h in cat. 3. In rat and man metabolism involves N-oxidation of the pyridine ring (Metabolite I), and in cat oxidation of the hydroxymethyl group (Metabolite II). Four other conjugated metabolites (III-VI) isolated from rat urine and bile, and from urine of cats and man, have been characterized. 4. The unchanged compound, but not its metabolites, crosses the blood-brain barrier in rat and cat. 5. The species differences in the disposition and metabolism of the compound are consistent with previous pharmacological data indicating a greater and more prolonged effect in cat.


Jan 1, 1971·Journal of Pharmaceutical Sciences·S Y Yeh, L A Woods


Jul 1, 1985·European Journal of Drug Metabolism and Pharmacokinetics·H AllarsR S Norton
Jan 1, 1985·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·P A DixonM C Enwelum

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