{"@context":{"@vocab":"https://cir.nii.ac.jp/schema/1.0/","rdfs":"http://www.w3.org/2000/01/rdf-schema#","dc":"http://purl.org/dc/elements/1.1/","dcterms":"http://purl.org/dc/terms/","foaf":"http://xmlns.com/foaf/0.1/","prism":"http://prismstandard.org/namespaces/basic/2.0/","cinii":"http://ci.nii.ac.jp/ns/1.0/","datacite":"https://schema.datacite.org/meta/kernel-4/","ndl":"http://ndl.go.jp/dcndl/terms/","jpcoar":"https://github.com/JPCOAR/schema/blob/master/2.0/"},"@id":"https://cir.nii.ac.jp/crid/1390282679474380672.json","@type":"Article","productIdentifier":[{"identifier":{"@type":"DOI","@value":"10.1248/jhs.52.623"}},{"identifier":{"@type":"NDL_BIB_ID","@value":"8073902"}},{"identifier":{"@type":"URI","@value":"http://id.ndl.go.jp/bib/8073902"}},{"identifier":{"@type":"URI","@value":"https://ndlsearch.ndl.go.jp/books/R000000004-I8073902"}},{"identifier":{"@type":"URI","@value":"https://dl.ndl.go.jp/pid/8717782"}},{"identifier":{"@type":"URI","@value":"http://www.jstage.jst.go.jp/article/jhs/52/5/52_5_623/_pdf"}},{"identifier":{"@type":"NAID","@value":"110004809618"}},{"identifier":{"@type":"URI","@value":"https://search.jamas.or.jp/link/ui/2007062911"}}],"dc:title":[{"@language":"en","@value":"Cytochrome P450 2E1/2A6-Selective Inhibition by Halogenated Anilines on Metabolic Activation of Dimethylnitrosamine in Human Liver Microsomes"}],"dc:language":"en","description":[{"type":"abstract","notation":[{"@language":"en","@value":"Nine halogenated anilines, consisting of di- and tri-substituted fluoro-, chloro-, and bromoanilines, were subjected to analysis of their cytochrome P450 (CYP) 2E1/2A6-selective inhibitory effects on metabolic activation of dimetylnitrosamine (DMN) in human liver microsomes. Inhibitory activities (IC<SUB>50</SUB>) of these anilines on human recombinant CYP2E1 ranged from 8.0 to 549 <I>μ</I>M. However, most of these anilines showed no remarkable inhibition of CYP1A2, while their IC<SUB>50</SUB> values on CYP2A6 ranged from 2.9 to 232 <I>μ</I>M. The CYP2E1 selectivity of these anilines in terms of the ratio of the IC<SUB>50</SUB> values of these anilines on CYP2A6 to those on CYP2E1, ranged from 0.1- to 5.2-fold. Their CYP2E1 selectivity decreased in the following order: 3,4,5-trifluoroaniline (3,4,5-triF-A) > 3,5-diF-A >> 3,5-dichloroaniline (3,5-diCl-A) > 3,4-diCl-A > 2,6-diCl-A > 2,3,4-trichloroaniline (2,3,4-triCl-A) > 2,4,6-triCl-A > 2,6-dibromoaniline (2,6-diBr-A) > 3,4,5-triCl-A. The inhibitory effects of these anilines on metabolic activation of DMN were analyzed using human liver microsomes. The IC<SUB>50</SUB> values of these anilines on demethylation metabolism of DMN correlated with those of these anilines on CYP2E1. These results suggest that these halogenated anilines may be useful as indicators of CYP-selectivity involved in metabolic activation of nitrosamines. <br>"}],"abstractLicenseFlag":"disallow"}],"creator":[{"@id":"https://cir.nii.ac.jp/crid/1410282679474380675","@type":"Researcher","personIdentifier":[{"@type":"NRID","@value":"9000001645976"}],"foaf:name":[{"@language":"en","@value":"Ohashi Yohei"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Graduate School of Pharmaceutical Sciences, Nagoya City University"}]},{"@id":"https://cir.nii.ac.jp/crid/1410282679474380676","@type":"Researcher","foaf:name":[{"@language":"en","@value":"Kato Taka-aki"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Graduate School of Pharmaceutical Sciences, Nagoya City 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Katsuya"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Graduate School of Pharmaceutical Sciences, Nagoya City University"}]},{"@id":"https://cir.nii.ac.jp/crid/1030003658325924992","@type":"Researcher","personIdentifier":[{"@type":"KAKEN_RESEARCHERS","@value":"30080188"},{"@type":"NRID","@value":"1000030080188"},{"@type":"NRID","@value":"9000005258231"},{"@type":"NRID","@value":"9000254698512"},{"@type":"NRID","@value":"9000006731667"},{"@type":"NRID","@value":"9000254680453"},{"@type":"NRID","@value":"9000391621135"},{"@type":"NRID","@value":"9000005130764"},{"@type":"NRID","@value":"9000254218369"},{"@type":"NRID","@value":"9000254215837"},{"@type":"NRID","@value":"9000391654888"},{"@type":"NRID","@value":"9000254213207"},{"@type":"NRID","@value":"9000254688273"},{"@type":"NRID","@value":"9000254680481"},{"@type":"NRID","@value":"9000006252392"},{"@type":"NRID","@value":"9000006405538"},{"@type":"NRID","@value":"9000254679385"},{"@type":"NRID","@value":"9000252817274"},{"@type":"NRID","@value":"9000258576277"},{"@type":"NRID","@value":"9000254218414"},{"@type":"NRID","@value":"9000254683873"},{"@type":"NRID","@value":"9000253203954"},{"@type":"NRID","@value":"9000253195444"},{"@type":"NRID","@value":"9000253192099"},{"@type":"NRID","@value":"9000006174888"},{"@type":"NRID","@value":"9000006405510"},{"@type":"NRID","@value":"9000254220257"},{"@type":"NRID","@value":"9000254679167"},{"@type":"NRID","@value":"9000391657696"},{"@type":"NRID","@value":"9000391655046"},{"@type":"NRID","@value":"9000254686259"},{"@type":"NRID","@value":"9000258576284"},{"@type":"NRID","@value":"9000259297026"},{"@type":"NRID","@value":"9000253192696"},{"@type":"NRID","@value":"9000257967108"},{"@type":"NRID","@value":"9000005262890"},{"@type":"NRID","@value":"9000254681363"},{"@type":"NRID","@value":"9000254683107"},{"@type":"NRID","@value":"9000254680652"},{"@type":"NRID","@value":"9000391655048"},{"@type":"NRID","@value":"9000254678122"},{"@type":"NRID","@value":"9000254222497"}],"foaf:name":[{"@language":"en","@value":"Mizutani Takaharu"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Graduate School of Pharmaceutical Sciences, Nagoya City University"}]},{"@id":"https://cir.nii.ac.jp/crid/1420001326233582464","@type":"Researcher","personIdentifier":[{"@type":"KAKEN_RESEARCHERS","@value":"60254306"},{"@type":"NRID","@value":"1000060254306"},{"@type":"NRID","@value":"9000003006962"},{"@type":"NRID","@value":"9000020281026"},{"@type":"NRID","@value":"9000023070903"},{"@type":"NRID","@value":"9000018667756"},{"@type":"NRID","@value":"9000258571774"},{"@type":"NRID","@value":"9000005255680"},{"@type":"NRID","@value":"9000237725836"},{"@type":"NRID","@value":"9000392642730"},{"@type":"NRID","@value":"9000005235073"},{"@type":"NRID","@value":"9000005270785"},{"@type":"NRID","@value":"9000258573338"},{"@type":"NRID","@value":"9000010083981"},{"@type":"NRID","@value":"9000006405561"},{"@type":"RESEARCHMAP","@value":"https://researchmap.jp/read0043851"}],"foaf:name":[{"@language":"en","@value":"Saeki Ken-ichi"}],"jpcoar:affiliationName":[{"@language":"en","@value":"Graduate School of Pharmaceutical Sciences, Nagoya City University"}]}],"publication":{"publicationIdentifier":[{"@type":"PISSN","@value":"13449702"},{"@type":"EISSN","@value":"13475207"},{"@type":"CODEN","@value":"JHSCFD"},{"@type":"NDL_BIB_ID","@value":"000000160750"},{"@type":"ISSN","@value":"13449702"},{"@type":"LISSN","@value":"13449702"},{"@type":"NCID","@value":"AA11316464"}],"prism:publicationName":[{"@language":"ja","@value":"ＪＯＵＲＮＡＬ　ＯＦ　ＨＥＡＬＴＨ　ＳＣＩＥＮＣＥ"},{"@language":"en","@value":"Journal of Health Science"},{"@language":"en","@value":"JOURNAL OF HEALTH SCIENCE"},{"@language":"en","@value":"J. Health Sci."},{"@language":"ja","@value":"Ｊ．　Ｈｅａｌｔｈ　Ｓｃｉ．"}],"dc:publisher":[{"@language":"en","@value":"The Pharmaceutical Society of Japan"},{"@language":"ja","@value":"公益社団法人 日本薬学会"}],"prism:publicationDate":"2006","prism:volume":"52","prism:number":"5","prism:startingPage":"623","prism:endingPage":"627"},"reviewed":"false","dcterms:accessRights":"http://purl.org/coar/access_right/c_abf2","url":[{"@id":"http://id.ndl.go.jp/bib/8073902"},{"@id":"https://ndlsearch.ndl.go.jp/books/R000000004-I8073902"},{"@id":"https://dl.ndl.go.jp/pid/8717782"},{"@id":"http://www.jstage.jst.go.jp/article/jhs/52/5/52_5_623/_pdf"},{"@id":"https://search.jamas.or.jp/link/ui/2007062911"}],"availableAt":"2006","foaf:topic":[{"@id":"https://cir.nii.ac.jp/all?q=inhibitor","dc:title":"inhibitor"},{"@id":"https://cir.nii.ac.jp/all?q=halogen-substitution","dc:title":"halogen-substitution"},{"@id":"https://cir.nii.ac.jp/all?q=cytochrome%20P450%202E1","dc:title":"cytochrome P450 2E1"},{"@id":"https://cir.nii.ac.jp/all?q=alkylnitrosamine","dc:title":"alkylnitrosamine"},{"@id":"https://cir.nii.ac.jp/all?q=carcinogenicity","dc:title":"carcinogenicity"}],"relatedProduct":[{"@id":"https://cir.nii.ac.jp/crid/1360292619593581696","@type":"Article","relationType":["references"],"jpcoar:relatedTitle":[{"@value":"Cytochrome P450 species involved in the metabolism of\nquinoline"}]},{"@id":"https://cir.nii.ac.jp/crid/1360574096140319744","@type":"Article","relationType":["references","cites"],"jpcoar:relatedTitle":[{"@value":"High variability of nitrosamine metabolism among individuals: Role of cytochromes P450 2A6 and 2E1 in the dealkylation of <i>N</i>‐nitrosodimethylamine and <i>N</i>‐nitrosodiethylamine in mice and humans"}]},{"@id":"https://cir.nii.ac.jp/crid/1361418519030839680","@type":"Article","relationType":["references"],"jpcoar:relatedTitle":[{"@value":"Cytochrome P450 2E1 and 2A6 enzymes as major catalysts for metabolic activation of 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