FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2019955239> ?p ?o ?g. }

• W2019955239 endingPage "1259" @default.
• W2019955239 startingPage "1252" @default.
• W2019955239 abstract "The aim of the present study was to identify cytochrome P450 (CYP) isoenzymes involved in the 5-sulfoxidation, mono-N-demethylation and di-N-demethylation of the aliphatic-type phenothiazine neuroleptic chlorpromazine in human liver. Experiments were performed in vitro using cDNA-expressed human CYP isoforms (Supersomes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4), liver microsomes from different donors and CYP-selective inhibitors. The obtained results indicate that CYP1A2 is the only CYP isoform that catalyzes the mono-N-demethylation and di-N-demethylation of chlorpromazine (100%) and is the main isoform responsible for chlorpromazine 5-sulfoxidation (64%) at a therapeutic concentration of the drug (10 microM). CYP3A4 contributes to a lesser degree to chlorpromazine 5-sulfoxidation (34%). The role of CYP2B6, CYP2C19 and CYP2D6 in catalyzing of the latter reaction is negligible (0.1-2%). Similar results were obtained at a higher, non-therapeutic concentration of the drug (100 microM); however, the contribution of CYP1A2 to chlorpromazine mono-N-demethylation was noticeably lower (75%), mostly in favour of CYP2C19 and CYP3A4 (about 12% each). The obtained results indicate that the catalysis of chlorpromazine N-demethylation and 5-sulfoxidation in humans exhibits a stricter CYP1A2 preference compared to the previously tested phenothiazines (promazine, perazine, and thioridazine). Hence pharmacokinetic interactions involving chlorpromazine and CYP1A2 substrates and inhibitors are likely to occur. Considering strong dopaminergic D(2), noradrenergic alpha(1) and cholinergic M(1) receptor blocking properties of chlorpromazine and some of its metabolites, as well as their serious side effects, the obtained results may be of pharmacological and clinical importance." @default.
• W2019955239 created "2016-06-24" @default.
• W2019955239 creator A5008157954 @default.
• W2019955239 creator A5047848223 @default.
• W2019955239 creator A5075074462 @default.
• W2019955239 date "2010-10-01" @default.
• W2019955239 modified "2023-10-12" @default.
• W2019955239 title "Main contribution of the cytochrome P450 isoenzyme 1A2 (CYP1A2) to N-demethylation and 5-sulfoxidation of the phenothiazine neuroleptic chlorpromazine in human liver—A comparison with other phenothiazines" @default.
• W2019955239 cites W1969652902 @default.
• W2019955239 cites W1995285447 @default.
• W2019955239 cites W1999243862 @default.
• W2019955239 cites W2017035076 @default.
• W2019955239 cites W2017651501 @default.
• W2019955239 cites W2024541179 @default.
• W2019955239 cites W2028211663 @default.
• W2019955239 cites W2039135632 @default.
• W2019955239 cites W2041472256 @default.
• W2019955239 cites W2058848060 @default.
• W2019955239 cites W2060756986 @default.
• W2019955239 cites W2066144752 @default.
• W2019955239 cites W2076807783 @default.
• W2019955239 cites W2094542356 @default.
• W2019955239 cites W2156445661 @default.
• W2019955239 cites W4292487048 @default.
• W2019955239 doi "https://doi.org/10.1016/j.bcp.2010.06.045" @default.
• W2019955239 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20615392" @default.
• W2019955239 hasPublicationYear "2010" @default.
• W2019955239 type Work @default.
• W2019955239 sameAs 2019955239 @default.
• W2019955239 citedByCount "54" @default.
• W2019955239 countsByYear W20199552392012 @default.
• W2019955239 countsByYear W20199552392013 @default.
• W2019955239 countsByYear W20199552392014 @default.
• W2019955239 countsByYear W20199552392015 @default.
• W2019955239 countsByYear W20199552392016 @default.
• W2019955239 countsByYear W20199552392017 @default.
• W2019955239 countsByYear W20199552392018 @default.
• W2019955239 countsByYear W20199552392019 @default.
• W2019955239 countsByYear W20199552392020 @default.
• W2019955239 countsByYear W20199552392021 @default.
• W2019955239 countsByYear W20199552392023 @default.
• W2019955239 crossrefType "journal-article" @default.
• W2019955239 hasAuthorship W2019955239A5008157954 @default.
• W2019955239 hasAuthorship W2019955239A5047848223 @default.
• W2019955239 hasAuthorship W2019955239A5075074462 @default.
• W2019955239 hasConcept C104317684 @default.
• W2019955239 hasConcept C109650736 @default.
• W2019955239 hasConcept C150194340 @default.
• W2019955239 hasConcept C181199279 @default.
• W2019955239 hasConcept C185592680 @default.
• W2019955239 hasConcept C190727270 @default.
• W2019955239 hasConcept C202199734 @default.
• W2019955239 hasConcept C2776484668 @default.
• W2019955239 hasConcept C2778716775 @default.
• W2019955239 hasConcept C2778775820 @default.
• W2019955239 hasConcept C2780688371 @default.
• W2019955239 hasConcept C2781109383 @default.
• W2019955239 hasConcept C33664856 @default.
• W2019955239 hasConcept C526171541 @default.
• W2019955239 hasConcept C55493867 @default.
• W2019955239 hasConcept C62231903 @default.
• W2019955239 hasConcept C71924100 @default.
• W2019955239 hasConcept C86745063 @default.
• W2019955239 hasConcept C87644729 @default.
• W2019955239 hasConcept C98274493 @default.
• W2019955239 hasConceptScore W2019955239C104317684 @default.
• W2019955239 hasConceptScore W2019955239C109650736 @default.
• W2019955239 hasConceptScore W2019955239C150194340 @default.
• W2019955239 hasConceptScore W2019955239C181199279 @default.
• W2019955239 hasConceptScore W2019955239C185592680 @default.
• W2019955239 hasConceptScore W2019955239C190727270 @default.
• W2019955239 hasConceptScore W2019955239C202199734 @default.
• W2019955239 hasConceptScore W2019955239C2776484668 @default.
• W2019955239 hasConceptScore W2019955239C2778716775 @default.
• W2019955239 hasConceptScore W2019955239C2778775820 @default.
• W2019955239 hasConceptScore W2019955239C2780688371 @default.
• W2019955239 hasConceptScore W2019955239C2781109383 @default.
• W2019955239 hasConceptScore W2019955239C33664856 @default.
• W2019955239 hasConceptScore W2019955239C526171541 @default.
• W2019955239 hasConceptScore W2019955239C55493867 @default.
• W2019955239 hasConceptScore W2019955239C62231903 @default.
• W2019955239 hasConceptScore W2019955239C71924100 @default.
• W2019955239 hasConceptScore W2019955239C86745063 @default.
• W2019955239 hasConceptScore W2019955239C87644729 @default.
• W2019955239 hasConceptScore W2019955239C98274493 @default.
• W2019955239 hasIssue "8" @default.
• W2019955239 hasLocation W20199552391 @default.
• W2019955239 hasLocation W20199552392 @default.
• W2019955239 hasOpenAccess W2019955239 @default.
• W2019955239 hasPrimaryLocation W20199552391 @default.
• W2019955239 hasRelatedWork W1926074819 @default.
• W2019955239 hasRelatedWork W1955866317 @default.
• W2019955239 hasRelatedWork W1966494170 @default.
• W2019955239 hasRelatedWork W2027268501 @default.
• W2019955239 hasRelatedWork W2057621776 @default.
• W2019955239 hasRelatedWork W2395395681 @default.
• W2019955239 hasRelatedWork W2402752673 @default.
• W2019955239 hasRelatedWork W2410724967 @default.

• next