Induction of rat-hepatic microsomal cytochrome P-450 and aryl hydrocarbon hydroxylase by 1,3-benzodioxole derivatives
1. Several 1,3-benzodioxoles (BD) and related compounds were studied in relation to their ability to generate metabolite complexes with hepatic cytochrome P-450 following administration in vivo to rats. 2. BD derivatives that formed stable metabolite complexes with cytochrome P-450 were considerably...
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| Veröffentlicht in: | Xenobiotica 1985-01, Vol.15 (5), p.361-368 |
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| creator | Murray, M. Wilkinso, C. F. Dube, C. E. |
| description | 1. Several 1,3-benzodioxoles (BD) and related compounds were studied in relation to their ability to generate metabolite complexes with hepatic cytochrome P-450 following administration in vivo to rats.
2. BD derivatives that formed stable metabolite complexes with cytochrome P-450 were considerably more effective inducers of cytochrome P-450 and aryl hydrocarbon (benzo[α]pyrene) hydroxylase (AHH) activity than derivatives that did not form stable complexes.
3. Linear regression analysis showed that AHH activity was well correlated (r = 0.980) with total (i.e. complexed plus uncomplexed) cytochrome P-450 content and was not correlated with levels of uncomplexed cytochrome P-450.
4. Aminopyrine N-demethylase (APDM) activity in hepatic microsomes from rats treated with 1,3-benzodioxoles was moderately correlated in a linear relationship with uncomplexed levels of cytochrome P-450 and not with total cytochrome P-450. |
| doi_str_mv | 10.3109/00498258509045006 |
| format | Article |
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2. BD derivatives that formed stable metabolite complexes with cytochrome P-450 were considerably more effective inducers of cytochrome P-450 and aryl hydrocarbon (benzo[α]pyrene) hydroxylase (AHH) activity than derivatives that did not form stable complexes.
3. Linear regression analysis showed that AHH activity was well correlated (r = 0.980) with total (i.e. complexed plus uncomplexed) cytochrome P-450 content and was not correlated with levels of uncomplexed cytochrome P-450.
4. Aminopyrine N-demethylase (APDM) activity in hepatic microsomes from rats treated with 1,3-benzodioxoles was moderately correlated in a linear relationship with uncomplexed levels of cytochrome P-450 and not with total cytochrome P-450.</description><identifier>ISSN: 0049-8254</identifier><identifier>EISSN: 1366-5928</identifier><identifier>DOI: 10.3109/00498258509045006</identifier><identifier>PMID: 4036164</identifier><identifier>CODEN: XENOBH</identifier><language>eng</language><publisher>London: Informa UK Ltd</publisher><subject>Aminopyrine N-Demethylase - metabolism ; Animals ; Aryl Hydrocarbon Hydroxylases - metabolism ; Biological and medical sciences ; Chemical and industrial products toxicology. Toxic occupational diseases ; Cytochrome P-450 Enzyme System - metabolism ; Dioxoles - metabolism ; Dioxoles - pharmacology ; Enzyme Induction - drug effects ; Isoenzymes - metabolism ; Male ; Medical sciences ; Microsomes, Liver - drug effects ; Microsomes, Liver - enzymology ; Rats ; Rats, Inbred Strains ; Structure-Activity Relationship ; Toxicology ; Various organic compounds</subject><ispartof>Xenobiotica, 1985-01, Vol.15 (5), p.361-368</ispartof><rights>1985 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1985</rights><rights>1986 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c430t-d00e2084aa6db90278b5a93684a1151e65f7f3e89ecaadc4f0118d779987c00a3</citedby><cites>FETCH-LOGICAL-c430t-d00e2084aa6db90278b5a93684a1151e65f7f3e89ecaadc4f0118d779987c00a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/00498258509045006$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/00498258509045006$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,777,781,27905,27906,59626,59732,60415,60521,61200,61235,61381,61416</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8408509$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/4036164$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Murray, M.</creatorcontrib><creatorcontrib>Wilkinso, C. F.</creatorcontrib><creatorcontrib>Dube, C. E.</creatorcontrib><title>Induction of rat-hepatic microsomal cytochrome P-450 and aryl hydrocarbon hydroxylase by 1,3-benzodioxole derivatives</title><title>Xenobiotica</title><addtitle>Xenobiotica</addtitle><description>1. Several 1,3-benzodioxoles (BD) and related compounds were studied in relation to their ability to generate metabolite complexes with hepatic cytochrome P-450 following administration in vivo to rats.
2. BD derivatives that formed stable metabolite complexes with cytochrome P-450 were considerably more effective inducers of cytochrome P-450 and aryl hydrocarbon (benzo[α]pyrene) hydroxylase (AHH) activity than derivatives that did not form stable complexes.
3. Linear regression analysis showed that AHH activity was well correlated (r = 0.980) with total (i.e. complexed plus uncomplexed) cytochrome P-450 content and was not correlated with levels of uncomplexed cytochrome P-450.
4. Aminopyrine N-demethylase (APDM) activity in hepatic microsomes from rats treated with 1,3-benzodioxoles was moderately correlated in a linear relationship with uncomplexed levels of cytochrome P-450 and not with total cytochrome P-450.</description><subject>Aminopyrine N-Demethylase - metabolism</subject><subject>Animals</subject><subject>Aryl Hydrocarbon Hydroxylases - metabolism</subject><subject>Biological and medical sciences</subject><subject>Chemical and industrial products toxicology. Toxic occupational diseases</subject><subject>Cytochrome P-450 Enzyme System - metabolism</subject><subject>Dioxoles - metabolism</subject><subject>Dioxoles - pharmacology</subject><subject>Enzyme Induction - drug effects</subject><subject>Isoenzymes - metabolism</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - enzymology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Structure-Activity Relationship</subject><subject>Toxicology</subject><subject>Various organic compounds</subject><issn>0049-8254</issn><issn>1366-5928</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1985</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kUFv1DAQhS1EVZbCD-CA5APi1NBxnDiJ6AVVBSpVKgc4RxN7orhy4sVOSsOvx9tdKiGknmz5fe_Z88zYGwEfpIDmDKBo6rysS2igKAHUM7YRUqmsbPL6Odvs9CwBxQv2MsZbSITI82N2XIBUQhUbtlxNZtGz9RP3PQ84ZwNtcbaaj1YHH_2Ijut19noIfiT-LUv3cJwMx7A6PqwmeI2hS_6H_f3qMBLvVi5OZdbR9Nsb6--9I24o2LsUfUfxFTvq0UV6fVhP2I_Pl98vvmbXN1-uLj5dZ7qQMGcGgHKoC0Rlugbyqu5KbKRKJ0KUglTZV72kuiGNaHTRgxC1qaqmqSsNgPKEvd_nboP_uVCc29FGTc7hRH6JbaWkKqu8SqDYg7uZY6C-3QY7phFbAe2u6va_qpPn7SF86UYyj45Dt0l_d9AxanR9wEnb-IjVBezCEna-x-zU-zDiLx-caWdcnQ9_PfKpV3z8xz4QunlIX0LtrV_ClOp9YoY_ZvKr_Q</recordid><startdate>19850101</startdate><enddate>19850101</enddate><creator>Murray, M.</creator><creator>Wilkinso, C. F.</creator><creator>Dube, C. E.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19850101</creationdate><title>Induction of rat-hepatic microsomal cytochrome P-450 and aryl hydrocarbon hydroxylase by 1,3-benzodioxole derivatives</title><author>Murray, M. ; Wilkinso, C. F. ; Dube, C. E.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c430t-d00e2084aa6db90278b5a93684a1151e65f7f3e89ecaadc4f0118d779987c00a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1985</creationdate><topic>Aminopyrine N-Demethylase - metabolism</topic><topic>Animals</topic><topic>Aryl Hydrocarbon Hydroxylases - metabolism</topic><topic>Biological and medical sciences</topic><topic>Chemical and industrial products toxicology. Toxic occupational diseases</topic><topic>Cytochrome P-450 Enzyme System - metabolism</topic><topic>Dioxoles - metabolism</topic><topic>Dioxoles - pharmacology</topic><topic>Enzyme Induction - drug effects</topic><topic>Isoenzymes - metabolism</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Microsomes, Liver - drug effects</topic><topic>Microsomes, Liver - enzymology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Structure-Activity Relationship</topic><topic>Toxicology</topic><topic>Various organic compounds</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Murray, M.</creatorcontrib><creatorcontrib>Wilkinso, C. F.</creatorcontrib><creatorcontrib>Dube, C. E.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Xenobiotica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Murray, M.</au><au>Wilkinso, C. F.</au><au>Dube, C. E.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Induction of rat-hepatic microsomal cytochrome P-450 and aryl hydrocarbon hydroxylase by 1,3-benzodioxole derivatives</atitle><jtitle>Xenobiotica</jtitle><addtitle>Xenobiotica</addtitle><date>1985-01-01</date><risdate>1985</risdate><volume>15</volume><issue>5</issue><spage>361</spage><epage>368</epage><pages>361-368</pages><issn>0049-8254</issn><eissn>1366-5928</eissn><coden>XENOBH</coden><abstract>1. Several 1,3-benzodioxoles (BD) and related compounds were studied in relation to their ability to generate metabolite complexes with hepatic cytochrome P-450 following administration in vivo to rats.
2. BD derivatives that formed stable metabolite complexes with cytochrome P-450 were considerably more effective inducers of cytochrome P-450 and aryl hydrocarbon (benzo[α]pyrene) hydroxylase (AHH) activity than derivatives that did not form stable complexes.
3. Linear regression analysis showed that AHH activity was well correlated (r = 0.980) with total (i.e. complexed plus uncomplexed) cytochrome P-450 content and was not correlated with levels of uncomplexed cytochrome P-450.
4. Aminopyrine N-demethylase (APDM) activity in hepatic microsomes from rats treated with 1,3-benzodioxoles was moderately correlated in a linear relationship with uncomplexed levels of cytochrome P-450 and not with total cytochrome P-450.</abstract><cop>London</cop><pub>Informa UK Ltd</pub><pmid>4036164</pmid><doi>10.3109/00498258509045006</doi><tpages>8</tpages></addata></record> |
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| identifier | ISSN: 0049-8254 |
| ispartof | Xenobiotica, 1985-01, Vol.15 (5), p.361-368 |
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| language | eng |
| recordid | cdi_pubmed_primary_4036164 |
| source | MEDLINE; Taylor & Francis Medical Library - CRKN; Taylor & Francis Journals Complete |
| subjects | Aminopyrine N-Demethylase - metabolism Animals Aryl Hydrocarbon Hydroxylases - metabolism Biological and medical sciences Chemical and industrial products toxicology. Toxic occupational diseases Cytochrome P-450 Enzyme System - metabolism Dioxoles - metabolism Dioxoles - pharmacology Enzyme Induction - drug effects Isoenzymes - metabolism Male Medical sciences Microsomes, Liver - drug effects Microsomes, Liver - enzymology Rats Rats, Inbred Strains Structure-Activity Relationship Toxicology Various organic compounds |
| title | Induction of rat-hepatic microsomal cytochrome P-450 and aryl hydrocarbon hydroxylase by 1,3-benzodioxole derivatives |
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