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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
12
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pubmed:dateCreated |
1991-8-27
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pubmed:abstractText |
The enantiomer specific pharmacokinetics of ring substituted warfarin analogues have been studied in the rat after the administration of 2 mg kg-1 of the racemates. The stereoselective differences observed were due to stereoselective plasma protein binding and stereoselective intrinsic hepatic clearance. Greater binding was observed for the S-enantiomers except for 2'-substituted analogues where the R-enantiomers were more tightly bound. The stereoselectivity in the binding ranged up to a factor of about 4. All substituted warfarins showed a higher intrinsic clearance than warfarin. Enantiomer selectivity depended on the position of the substituent; warfarin and 3'-substituted analogues showed R greater than S; 4'- and 2' substituted warfarins showed S greater than R stereoselectivity. Exceptions to this generality were seen for 4'- methoxy- and 4'-methylwarfarin which did not show stereoselective hepatic clearance.
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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 |
Dec
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pubmed:issn |
0022-3573
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
42
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
861-6
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:1983149-Animals,
pubmed-meshheading:1983149-Blood Proteins,
pubmed-meshheading:1983149-Chromatography, High Pressure Liquid,
pubmed-meshheading:1983149-Half-Life,
pubmed-meshheading:1983149-Male,
pubmed-meshheading:1983149-Protein Binding,
pubmed-meshheading:1983149-Rats,
pubmed-meshheading:1983149-Rats, Inbred Strains,
pubmed-meshheading:1983149-Stereoisomerism,
pubmed-meshheading:1983149-Structure-Activity Relationship,
pubmed-meshheading:1983149-Warfarin
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pubmed:year |
1990
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pubmed:articleTitle |
Enantioselective structure-pharmacokinetic relationships of ring substituted warfarin analogues in the rat.
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pubmed:affiliation |
Dept of Pharmacology, University of Limburg, Maastricht, The Netherlands.
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pubmed:publicationType |
Journal Article
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