Document Detail


Structure determination of metabolites of rilmazafone, a 1H-1,2,4-triazolyl benzophenone derivative in monkey urine.
MedLine Citation:
PMID:  3381539     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1. The metabolism of a new hypnotic 5-[(2-aminoacetamido)methyl]- 1-[4-chloro-2-(o-chlorobenzoyl)phenyl]-N,N-dimethyl-1H-1,2,4-tr iaz ole-3-carboxamide hydrochloride dihydrate (rilmazafone hydrochloride) was studies in female cynomolgus monkeys. 2. The structures of ten urinary metabolites were determined by mass spectrometry, and confirmed by comparison with synthetic authentic compounds. 3. Pathways of metabolism are postulated indicating that rilmazafone is desglycylated and cyclized to M-1, demethylated successively to M-2 and M-3, then hydrolysed to M-4, or hydroxylated at the 4-position of benzodiazepine ring or the p-position of the o-chlorophenyl group.
Authors:
M Koike; R Norikura; K Iwatani; K Sugeno; S Takahashi; Y Nakagawa
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Xenobiotica; the fate of foreign compounds in biological systems     Volume:  18     ISSN:  0049-8254     ISO Abbreviation:  Xenobiotica     Publication Date:  1988 Mar 
Date Detail:
Created Date:  1988-07-19     Completed Date:  1988-07-19     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  1306665     Medline TA:  Xenobiotica     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  257-68     Citation Subset:  IM    
Affiliation:
Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.
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MeSH Terms
Descriptor/Qualifier:
Animals
Chemical Phenomena
Chemistry
Cyclization
Female
Hydroxylation
Hypnotics and Sedatives / metabolism*
Macaca fascicularis
Mass Spectrometry
Molecular Conformation
Triazoles / urine*
Chemical
Reg. No./Substance:
0/Hypnotics and Sedatives; 0/Triazoles; 99593-25-6/rilmazafone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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