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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1988-4-7
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pubmed:abstractText |
Conjugation of racemic E-10-hydroxynortriptyline (E-10-OH-NT) with glucuronic acid was studied in the liver microsomal fraction of rats and humans. The diastereomeric glucuronides of E-10-OH-NT were resolved and quantitated by HPLC. Only the (+)-enantiomer was glucuronidated in liver microsomes from humans. Rat liver microsomes catalyzed the formation of both glucuronides. Phenobarbital pretreatment of rats increased the glucuronidation of both enantiomers about five-fold. The formation rate of (+)-E-10-OH-NT glucuronide varied from 5.5 to 33.2 pmol/mg x min, in microsomes from 13 humans. High activity was found in individuals previously treated with pentobarbital. Inhibition experiments with human liver microsomes showed that amitriptyline is a potent competitive inhibitor of (+)-E-10-OH-NT glucuronidation. p-Nitrophenol, paracetamol and 2-hydroxydesipramine also inhibited this reaction.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0901-9928
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
61
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
335-41
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3125532-Adult,
pubmed-meshheading:3125532-Animals,
pubmed-meshheading:3125532-Chromatography, High Pressure Liquid,
pubmed-meshheading:3125532-Female,
pubmed-meshheading:3125532-Glucuronates,
pubmed-meshheading:3125532-Glucuronosyltransferase,
pubmed-meshheading:3125532-Humans,
pubmed-meshheading:3125532-Male,
pubmed-meshheading:3125532-Microsomes, Liver,
pubmed-meshheading:3125532-Middle Aged,
pubmed-meshheading:3125532-Nortriptyline,
pubmed-meshheading:3125532-Rats,
pubmed-meshheading:3125532-Rats, Inbred Strains,
pubmed-meshheading:3125532-Species Specificity,
pubmed-meshheading:3125532-Stereoisomerism
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pubmed:year |
1987
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pubmed:articleTitle |
Glucuronidation of the enantiomers of E-10-hydroxynortriptyline in human and rat liver microsomes.
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pubmed:affiliation |
Department of Clinical Pharmacology, Karolinska Institute, Huddinge University Hospital, Sweden.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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