Source:http://linkedlifedata.com/resource/pubmed/id/11746816
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
2001-12-17
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pubmed:abstractText |
Flobufen (F), a new antiinflammatory drug, has one chiral and one prochiral center in its structure. Reduction of rac-F, the principal biotransformation pathway, leads to the formation of four diastereoisomers of 4-dihydroflobufen (DHF). F was chosen as a model substrate for interspecies comparison of activity, stereospecificity, and stereoselectivity of biotransformation enzymes in fallow bucks, red deer stags, and roe bucks in vitro. Formation of F metabolites was examined in hepatocyte suspension and in subcellular fractions of liver homogenate. (+)-R-F, (-)-S-F and rac-F were used as substrates. After incubation of substrates, the amounts and ratios of DHF diastereoisomers and F enantiomers were assessed by HPLC, with (R,R)-ULMO and terguride-bonded columns. Considerable interspecies differences in stereoselectivity and stereospecificity of F reductases were found at the cellular and subcellular levels, although these ruminants are closely related. Chiral inversion of F enantiomers to their antipodes was detected in vitro in all ruminants tested, but individual species also differed in the direction and rate of this inversion.
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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:issn |
0899-0042
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2001 Wiley-Liss, Inc.
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pubmed:issnType |
Print
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
760-4
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11746816-Animals,
pubmed-meshheading:11746816-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:11746816-Butyric Acids,
pubmed-meshheading:11746816-Cytosol,
pubmed-meshheading:11746816-Deer,
pubmed-meshheading:11746816-Hepatocytes,
pubmed-meshheading:11746816-Male,
pubmed-meshheading:11746816-Microsomes, Liver,
pubmed-meshheading:11746816-Oxidation-Reduction,
pubmed-meshheading:11746816-Species Specificity,
pubmed-meshheading:11746816-Stereoisomerism
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pubmed:year |
2001
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pubmed:articleTitle |
Biotransformation of flobufen enantiomers in ruminant hepatocytes and subcellular fractions.
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pubmed:affiliation |
Department of Biochemical Sciences, Faculty of Pharmacy, Research Centre LN 00B125, Charles University, Hradec Králové, Czech Republic. SKAOVAL@FAF.CUNI.CZ
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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