Matches in SemOpenAlex for { <https://semopenalex.org/work/W1982204329> ?p ?o ?g. }
Showing items 1 to 86 of
86
with 100 items per page.
- W1982204329 endingPage "417" @default.
- W1982204329 startingPage "405" @default.
- W1982204329 abstract "The identification and relative contribution of human cytochrome P450 enzyme(s) involved in the metabolism of SCH 351125 were investigated. In human liver microsomes, O-deethylation was the major metabolic pathway, whereas aromatization of a piperidine ring to pyridine and the reduction of the N-oxide moiety were minor routes. Recombinant human CYP3A4 and CYP2C9 both exhibited catalytic activity with respect to the formation of rotameric O-deethylated metabolites (M12, M13), the metabolites resulting from aromatization (M22/M24) and N-oxide reduction (M31). Using the relative activity factor (RAF) approach, the relative contributions of CYP3A4 and CYP2C9 to M13 formation were estimated to be 76 and 24%, respectively. There was a high correlation (r > 0.96) between the rate of formation of M12 and M13 and 6β-hydroxylation of testosterone catalysed by CYP3A4/5. Ketoconazole (2 µM) and CYP3A4/5-specific inhibitory monoclonal antibody inhibited the formation of M12 and M13 from human liver microsomes by approximately 60 and 71%, respectively. The results demonstrate that the in vitro metabolism of SCH 351125 is mediated primarily via CYP3A4 and that CYP2C9 plays a minor role. Clinical study designs should encompass these enzymology data to address any potential drug interactions." @default.
- W1982204329 created "2016-06-24" @default.
- W1982204329 creator A5001381737 @default.
- W1982204329 creator A5005525567 @default.
- W1982204329 creator A5009445940 @default.
- W1982204329 creator A5012621958 @default.
- W1982204329 creator A5024201441 @default.
- W1982204329 creator A5026276190 @default.
- W1982204329 creator A5048320268 @default.
- W1982204329 creator A5073618545 @default.
- W1982204329 creator A5079338576 @default.
- W1982204329 date "2005-05-01" @default.
- W1982204329 modified "2023-10-17" @default.
- W1982204329 title "Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 351125, a CCR5 antagonist" @default.
- W1982204329 cites W1568250830 @default.
- W1982204329 cites W161985329 @default.
- W1982204329 cites W2006998778 @default.
- W1982204329 cites W2015089407 @default.
- W1982204329 cites W2048289851 @default.
- W1982204329 cites W2085583693 @default.
- W1982204329 cites W4234857678 @default.
- W1982204329 doi "https://doi.org/10.1080/00498250500136569" @default.
- W1982204329 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16012074" @default.
- W1982204329 hasPublicationYear "2005" @default.
- W1982204329 type Work @default.
- W1982204329 sameAs 1982204329 @default.
- W1982204329 citedByCount "5" @default.
- W1982204329 countsByYear W19822043292014 @default.
- W1982204329 crossrefType "journal-article" @default.
- W1982204329 hasAuthorship W1982204329A5001381737 @default.
- W1982204329 hasAuthorship W1982204329A5005525567 @default.
- W1982204329 hasAuthorship W1982204329A5009445940 @default.
- W1982204329 hasAuthorship W1982204329A5012621958 @default.
- W1982204329 hasAuthorship W1982204329A5024201441 @default.
- W1982204329 hasAuthorship W1982204329A5026276190 @default.
- W1982204329 hasAuthorship W1982204329A5048320268 @default.
- W1982204329 hasAuthorship W1982204329A5073618545 @default.
- W1982204329 hasAuthorship W1982204329A5079338576 @default.
- W1982204329 hasConcept C109650736 @default.
- W1982204329 hasConcept C161790260 @default.
- W1982204329 hasConcept C181199279 @default.
- W1982204329 hasConcept C185592680 @default.
- W1982204329 hasConcept C2779325354 @default.
- W1982204329 hasConcept C2781109383 @default.
- W1982204329 hasConcept C526171541 @default.
- W1982204329 hasConcept C55493867 @default.
- W1982204329 hasConcept C62231903 @default.
- W1982204329 hasConcept C71240020 @default.
- W1982204329 hasConcept C86803240 @default.
- W1982204329 hasConcept C87644729 @default.
- W1982204329 hasConcept C89311334 @default.
- W1982204329 hasConceptScore W1982204329C109650736 @default.
- W1982204329 hasConceptScore W1982204329C161790260 @default.
- W1982204329 hasConceptScore W1982204329C181199279 @default.
- W1982204329 hasConceptScore W1982204329C185592680 @default.
- W1982204329 hasConceptScore W1982204329C2779325354 @default.
- W1982204329 hasConceptScore W1982204329C2781109383 @default.
- W1982204329 hasConceptScore W1982204329C526171541 @default.
- W1982204329 hasConceptScore W1982204329C55493867 @default.
- W1982204329 hasConceptScore W1982204329C62231903 @default.
- W1982204329 hasConceptScore W1982204329C71240020 @default.
- W1982204329 hasConceptScore W1982204329C86803240 @default.
- W1982204329 hasConceptScore W1982204329C87644729 @default.
- W1982204329 hasConceptScore W1982204329C89311334 @default.
- W1982204329 hasIssue "5" @default.
- W1982204329 hasLocation W19822043291 @default.
- W1982204329 hasLocation W19822043292 @default.
- W1982204329 hasOpenAccess W1982204329 @default.
- W1982204329 hasPrimaryLocation W19822043291 @default.
- W1982204329 hasRelatedWork W1764267039 @default.
- W1982204329 hasRelatedWork W1988026737 @default.
- W1982204329 hasRelatedWork W2014199317 @default.
- W1982204329 hasRelatedWork W2037012505 @default.
- W1982204329 hasRelatedWork W2063963014 @default.
- W1982204329 hasRelatedWork W2069896623 @default.
- W1982204329 hasRelatedWork W2138442990 @default.
- W1982204329 hasRelatedWork W2150393939 @default.
- W1982204329 hasRelatedWork W2370308986 @default.
- W1982204329 hasRelatedWork W2398565833 @default.
- W1982204329 hasVolume "35" @default.
- W1982204329 isParatext "false" @default.
- W1982204329 isRetracted "false" @default.
- W1982204329 magId "1982204329" @default.
- W1982204329 workType "article" @default.