Linked Life Data

15151171

Source:http://linkedlifedata.com/resource/pubmed/id/15151171

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2004-5-20
pubmed:abstractText
Glucosylation of xenobiotics in mammals has been observed for a limited number of drugs. Generally, these glucoside conjugates are detected as urinary excretion products with limited information on their formation. An in vitro assay is described for measuring the formation of the phenobarbital N-glucoside diasteriomers ((5R)-PBG, (5S)-PBG) using human liver microsomes. Human livers (n = 18) were screened for their ability to N-glucosylate PB. Cell viability, period of liver storage, prior drug exposure, serum bilirubin levels, age, sex and ethnicity did not appear to influence the specific activities associated with the formation of the PB N-glucosides. The average rate of formation for both PB N-glucoside was 1.42 +/- 1.04 (range 0.11-4.64) picomole/min/mg-protein with an (5S)-PBG/(5R)-PBG ratio of 6.75 +/- 1.34. The apparent kinetic constants, Km and Vmax, for PB N-glucosylation for eight of the livers ranged from 0.61-20.8 mM and 2.41-6.29 picomole/min/mg-protein, respectively. The apparent Vmax/Km ratio for PB exhibited a greater than 20 fold variation in the ability of the microsomes to form the PB N-glucosides. It would appear that the formation of these barbiturate N-glucoside conjugates in vitro are consistent with the amount of barbiturate N-glucosides formed and excreted in the urine in prior drug disposition studies.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0378-7966
pubmed:author
pubmed:issnType
Print
pubmed:volume
29
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
51-9
pubmed:dateRevised
2011-2-2
pubmed:meshHeading
pubmed:articleTitle
Phenobarbital N-glucosylation by human liver microsomes.
pubmed:affiliation
Department of Medicinal Chemistry, Medical College of Virginia/Virginia Commonwealth University, Richmond, USA.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, Non-P.H.S.