Source:http://linkedlifedata.com/resource/pubmed/id/12956899
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
8
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pubmed:dateCreated |
2003-9-5
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pubmed:abstractText |
The in-vitro biotransformation of the anxiolytic agent, RWJ-50172 was studied after incubation with rat hepatic S9 fraction in the presence of an NADPH-generating system, and incubating with Cunninghamella echinulata in soy-bean medium. Unchanged RWJ-50172 (80% of the sample in rat; 86% in fungi) plus 6 metabolites (M1-M6) were profiled, quantified and tentatively identified on the basis of API-MS/MS data. The metabolic pathways for RWJ-50172 are proposed, and the four metabolic pathways are: pyrido-oxidation (pathway A), phenylhydroxylation (B), dehydration (C) and reduction (D). Pathway A formed hydroxy-pyrido-RWJ-50172 (M1, 10% of the sample in both rat and fungi) as the only major metabolite, which further dehydrated to form dehydro-RWJ-50172 in trace quantities in rat. Pathway B produced hydroxyphenyl-RWJ-50172 (M2) in small amounts (4%) in rat, and in conjunction with step A formed dihydroxy-RWJ-50172 as a trace metabolite in rat. Step D produced a minor benzimidazole-reduced metabolite in fungi. RWJ-50172 is substantially metabolized by this rat hepatic S9 fraction and fungi.
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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 |
Aug
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pubmed:issn |
0022-3573
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
55
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1099-105
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12956899-Amides,
pubmed-meshheading:12956899-Animals,
pubmed-meshheading:12956899-Anti-Anxiety Agents,
pubmed-meshheading:12956899-Benzimidazoles,
pubmed-meshheading:12956899-Biotransformation,
pubmed-meshheading:12956899-Cunninghamella,
pubmed-meshheading:12956899-Male,
pubmed-meshheading:12956899-Microsomes, Liver,
pubmed-meshheading:12956899-Rats,
pubmed-meshheading:12956899-Rats, Sprague-Dawley
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pubmed:year |
2003
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pubmed:articleTitle |
In-vitro metabolism of the new anxiolytic agent, RWJ-50172, in rat hepatic S9 fraction and microbial transformation in fungi, Cunninghamella sp.
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pubmed:affiliation |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Spring House, PA 19477, USA. wwu@prdus.jnj.com
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pubmed:publicationType |
Journal Article,
In Vitro
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