Document Detail


Main metabolites of 1-(2-chloroethyl)-3-[1'-(5'-p-nitrobenzoyl-2',3'-isopropylidene)-alpha, beta-D-ribofuranosyl]-1-nitrosourea and 1-(2-chloroethyl)-3-(2',3', 4'-tri-O-acetyl-alpha, beta-D-ribopyranosyl)-1-nitrosourea in rats.
MedLine Citation:
PMID:  6130919     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The metabolism of two glycosylnitrosoureas, 1-(2-chloroethyl)-3-[1'-(5'-p-nitrobenzoyl-2',3'-isopropylidene)-alpha, beta-D-ribofuranosyl]-1-nitrosourea (RFCNU) and 1-(2-chloroethyl)-3-(2',3',4'-tri-O-acetyl-alpha, beta-D-ribopyranosyl)-1-nitrosourea (RPCNU), has been investigated in the rat. With the label on the carboxyl moiety of RFCNU, we have shown that hydrolysis of the 4-nitrobenzoyl ester occurred to a large extent in vivo; 4-nitrobenzoic acid and its glucuronide were the major urinary metabolites. Two other minor metabolites and their glucuronides were identified as 4-aminobenzoic acid and 4-acetamidobenzoic acid. With the label on the chloroethyl moieties of RFCNU and RPCNU, we have shown that chloroethanol was a major degradation product of this alkylating part of the molecule. The concentration of chloroethanol in plasma vs. time has been determined. In urine, four metabolites derived from alkylated glutathione, namely thiodiacetic acid and its sulfoxide, N-acetylcarboxymethylcysteine, and N-acetylhydroxyethylcysteine, have been identified.
Authors:
J C Madelmont; M F Moreau; D Godeneche; J Duprat; R Plagne; G Meyniel
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Drug metabolism and disposition: the biological fate of chemicals     Volume:  10     ISSN:  0090-9556     ISO Abbreviation:  Drug Metab. Dispos.     Publication Date:    1982 Nov-Dec
Date Detail:
Created Date:  1983-04-15     Completed Date:  1983-04-15     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9421550     Medline TA:  Drug Metab Dispos     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  662-6     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Carbon Radioisotopes / diagnostic use
Isotope Labeling
Male
Nitrosourea Compounds / blood,  metabolism*,  urine
Rats
Rats, Inbred Strains
Chemical
Reg. No./Substance:
0/Carbon Radioisotopes; 0/Nitrosourea Compounds; 55102-43-7/ICIG 1163; 56194-22-0/RFCNU

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


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