7-Bromo-5-(2'-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one (I), a new tranquillizing agent: metabolism in rats

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
A L EkonomovY I Vikhlyaev

Abstract

1. After intraperitoneal injection of rats with the new benzodiazepine (compound I), four metabolites (compounds II, III, IV and V) were found in the urine. 2. Compound II was identified as 7-bromo-5-(2'-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one by comparison of g.l.c. and mass spectral properties of the metabolite and synthetic compound. 3. Mass spectra of compound III and its acid hydrolysis products indicate that compound III contains a hydroxyl group in the C(5)-phenyl ring. 4. Compounds IV and V were identified by mass spectrometry as products of simultaneous aromatic hydroxylation and methoxylation of the diazepine I. 5. The major urinary excretion products are compounds III, IV and V. Only very small amounts of compounds I and II were detected.

References

Jul 8, 1971·Journal of Chromatography·A ForgioneG C Jommi
May 1, 1970·Journal of Medicinal Chemistry·W adée
Jan 1, 1971·Journal of Pharmaceutical Sciences·W Sadée, E Van der Kleijn
May 1, 1968·Journal of Medicinal Chemistry·S C BellM I Gluckman

Citations

Jan 1, 1982·European Journal of Drug Metabolism and Pharmacokinetics·V P ZherdevA L Ekonomov
Aug 25, 2015·Forensic Science International : Synergy·Koji YamaguchiYoukichi Ohno
Mar 13, 2012·Human Psychopharmacology·John M CorkeryAbdol Hamid Ghodse

Related Concepts

Benzodiazepinones
Metabolic Biotransformation
Anti-Anxiety Effect

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