Nov 1, 1975

Comparative biotransformation of triflubazam in rats, dogs, and monkeys

Drug Metabolism and Disposition : the Biological Fate of Chemicals
K B AltonJ L McGuire

Abstract

The biotransformation of 14C-triflubazam (ORF 8063; 1-methyl-5-phenyl-7-trifluoromethyl-1H-1,5-benzodiazepin-2-4-[3H,5H]-dione) was investigated in rats, dogs, and monkeys. Urinary metabolites, representing 65, 74, and 87%, respectively, of the total urinary radioactivity excreted by these three species, were isolated by preparative layer chromatography and characterized by various spectral techniques including gas chromatography/mass spectrometry, solid probe mass spectrometry, polarimetry, and infrared and nuclear magnetic resonance spectrometry. No parent drug was found in the urine of any species. Four metabolites were isolated from the rat including the 4'-hydroxyphenyl, dihydrodiol, and 3'-methoxy-4'hydroxy derivatives. N-demethylated metabolites were not isolated from rat urine. Five metabolites were isolated from dog urine, including 4-hydroxyphenyl, dihydrodiol, and catechol derivatives of triflubazam. Unlike the case of the rat, a catechol-O-methyl ether was not detected in dog urine. Six metabolites were isolated from monkey urine. The only major difference in metabolism in the monkey was the existence of both the dihydrodiol and N-desmethyldihydrodiol metabolites. No catechol-0-methyl ether was detected in monkey ur...Continue Reading

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Mentioned in this Paper

Metabolic Process, Cellular
Dione
Urine
Arene
Derivatives
Phenyl
Anti-Anxiety Effect
trans-1,2-dihydro-1,2-naphthalenediol
Chromatography
Methyl ether

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