Document Detail


Glucuronidation of labetalol at the two hydroxy positions by bovine liver microsomes. Isolation, purification, and structure elucidation of the glucuronides of labetalol.
MedLine Citation:
PMID:  1673399     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Glucuronidation is known to be a major metabolic pathway for labetalol. As the drug contains a phenolic and an alcoholic hydroxy group, in principle two regio isomeric glucuronides can be formed. By incubating the substrate labetalol with bovine liver microsomes, in the presence of the co-substrate UDP-glucuronic acid, both hydroxy positions were glucuronidated. The different glucuronides were isolated from the incubation mixture using Bond-Elut extraction cartridges and separated by means of high performance liquid chromatography. The formation of glucuronides was confirmed by performing reference incubations using radiolabeled UDP-glucuronic acid. Structure elucidation of the various glucuronides was done by nuclear magnetic resonance, ultraviolet spectroscopy, and mass spectrometry.
Authors:
N R Niemeijer; T K Gerding; R A De Zeeuw
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Drug metabolism and disposition: the biological fate of chemicals     Volume:  19     ISSN:  0090-9556     ISO Abbreviation:  Drug Metab. Dispos.     Publication Date:    1991 Jan-Feb
Date Detail:
Created Date:  1991-05-30     Completed Date:  1991-05-30     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:  20-3     Citation Subset:  IM    
Affiliation:
Laboratory Diephuis, Groningen, The Netherlands.
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MeSH Terms
Descriptor/Qualifier:
Animals
Cattle
Chromatography, High Pressure Liquid
Glucuronates / isolation & purification,  metabolism
Labetalol / metabolism*
Magnetic Resonance Spectroscopy
Mass Spectrometry
Microsomes, Liver / metabolism*
Spectrophotometry, Ultraviolet
Uridine Diphosphate Glucuronic Acid / metabolism
Chemical
Reg. No./Substance:
0/Glucuronates; 2616-64-0/Uridine Diphosphate Glucuronic Acid; 36894-69-6/Labetalol

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


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