Stereospecificity of Esterases Hydrolyzing Oxazepam Acetate
Esterases hydrolyzing the racemic acetate ester of the centrally acting drug oxazepam in mice were examined. Radiolabeled ester administered intravenously was hydrolyzed rapidly in the liver, kidneys, and brain. The distribution of the enzyme activity of liver and brain subcellular fractions was mea...
Gespeichert in:
| Veröffentlicht in: | Journal of pharmaceutical sciences 1978-09, Vol.67 (9), p.1208-1210 |
|---|---|
| Hauptverfasser: | , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 1210 |
|---|---|
| container_issue | 9 |
| container_start_page | 1208 |
| container_title | Journal of pharmaceutical sciences |
| container_volume | 67 |
| creator | Maksay, Gabor Tegyey, Zsuzsanna Ötvös, László |
| description | Esterases hydrolyzing the racemic acetate ester of the centrally acting drug oxazepam in mice were examined. Radiolabeled ester administered intravenously was hydrolyzed rapidly in the liver, kidneys, and brain. The distribution of the enzyme activity of liver and brain subcellular fractions was measured. Kinetic data and structure investigation of partially hydrolyzed racemic ester pointed to the stereoselectivity of liver and brain esterases. The preferred hydrolysis of the (R)-(−)-isomer in liver homogenates was attributed mainly to microsomal enzymes, while that of the (S)-(+)-isomer in brain was considered to be due to the mitochondrial fraction. This phenomenon was a common property of all species tested. |
| doi_str_mv | 10.1002/jps.2600670905 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_74149453</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0022354915422300</els_id><sourcerecordid>74149453</sourcerecordid><originalsourceid>FETCH-LOGICAL-c4925-a8bb532d379aeb2a2c7a0c5d86739a98c91cd5b611cedb3e4e1ef489a5be3e8a3</originalsourceid><addsrcrecordid>eNqFkElPwzAQRi3EVpYrJw45cUvxEiexOKGqlKWioII4Wo4zQYakCXYKpL8eoyAQB8RppJn3fdI8hA4IHhKM6fFT44Y0xjhOsMB8DQ0IpziMMUnW0cADNGQ8Ettox7kn7DHM-RbajAVOKRmgk3kLFmrXgDaF0abtgroIxs5vlQMXnHe5rctuZRaPwexdraBRVXCqoVUt7KGNQpUO9r_mLro_G9-NzsPpbHIxOp2GOhKUhyrNMs5ozhKhIKOK6kRhzfM0TphQItWC6JxnMSEa8oxBBASKKBWKZ8AgVWwXHfW9ja1fluBaWRmnoSzVAuqlk0lEIhFx5sFhD2pbO2ehkI01lbKdJFh-ypJelvyR5QOHX83LrIL8G-_t-LPoz2-mhO6fMnl5M_9VHfZZ412-f2eVfZb-74TLh-uJvLui5IbOb-XU82nPgzf5asBKpw0svBJjQbcyr81fX3wARFKYgg</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>74149453</pqid></control><display><type>article</type><title>Stereospecificity of Esterases Hydrolyzing Oxazepam Acetate</title><source>MEDLINE</source><source>Wiley Online Library Journals Frontfile Complete</source><source>Alma/SFX Local Collection</source><creator>Maksay, Gabor ; Tegyey, Zsuzsanna ; Ötvös, László</creator><creatorcontrib>Maksay, Gabor ; Tegyey, Zsuzsanna ; Ötvös, László</creatorcontrib><description>Esterases hydrolyzing the racemic acetate ester of the centrally acting drug oxazepam in mice were examined. Radiolabeled ester administered intravenously was hydrolyzed rapidly in the liver, kidneys, and brain. The distribution of the enzyme activity of liver and brain subcellular fractions was measured. Kinetic data and structure investigation of partially hydrolyzed racemic ester pointed to the stereoselectivity of liver and brain esterases. The preferred hydrolysis of the (R)-(−)-isomer in liver homogenates was attributed mainly to microsomal enzymes, while that of the (S)-(+)-isomer in brain was considered to be due to the mitochondrial fraction. This phenomenon was a common property of all species tested.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.2600670905</identifier><identifier>PMID: 690821</identifier><language>eng</language><publisher>Washington: Elsevier Inc</publisher><subject>Animals ; Brain - enzymology ; Circular Dichroism ; Enzymes-esterases hydrolyzing oxazepam acetate in vivo and in vitro ; Enzymes—esterases hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined ; Esterases - metabolism ; Esterases-hydrolyzing oxazepam acetate in vivo and in vitro ; Esterases—hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined ; hydrolysis of acetate ester in vivo and in vitro ; Hydrolysis-oxazepam acetate in vivo and in vitro ; Hydrolysis—oxazepam acetate in vivo and in vitro stereospecificity of esterases determined ; In Vitro Techniques ; Kinetics ; Liver - enzymology ; Male ; Mice ; Molecular Conformation ; Oxazepam - analogs & derivatives ; Oxazepam - metabolism ; Oxazepam acetate-hydrolysis in vivo and in vitro ; Oxazepam acetate—hydrolysis in vivo and in vitro stereospecificity of esterases determined ; stereospecificity determined ; stereospecificity of esterases determined ; Stereospecificity-esterases hydrolyzing oxazepam acetate in vivo and in vitro ; Subcellular Fractions - enzymology ; Tranquilizers-oxazepam ; Tranquilizers—oxazepam hydrolysis of acetate ester in vivo and in vitro, stereospecificity of esterases determined</subject><ispartof>Journal of pharmaceutical sciences, 1978-09, Vol.67 (9), p.1208-1210</ispartof><rights>1978 Wiley-Liss, Inc., A Wiley Company</rights><rights>Copyright © 1978 Wiley‐Liss, Inc., A Wiley Company</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4925-a8bb532d379aeb2a2c7a0c5d86739a98c91cd5b611cedb3e4e1ef489a5be3e8a3</citedby><cites>FETCH-LOGICAL-c4925-a8bb532d379aeb2a2c7a0c5d86739a98c91cd5b611cedb3e4e1ef489a5be3e8a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.2600670905$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.2600670905$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/690821$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Maksay, Gabor</creatorcontrib><creatorcontrib>Tegyey, Zsuzsanna</creatorcontrib><creatorcontrib>Ötvös, László</creatorcontrib><title>Stereospecificity of Esterases Hydrolyzing Oxazepam Acetate</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>Esterases hydrolyzing the racemic acetate ester of the centrally acting drug oxazepam in mice were examined. Radiolabeled ester administered intravenously was hydrolyzed rapidly in the liver, kidneys, and brain. The distribution of the enzyme activity of liver and brain subcellular fractions was measured. Kinetic data and structure investigation of partially hydrolyzed racemic ester pointed to the stereoselectivity of liver and brain esterases. The preferred hydrolysis of the (R)-(−)-isomer in liver homogenates was attributed mainly to microsomal enzymes, while that of the (S)-(+)-isomer in brain was considered to be due to the mitochondrial fraction. This phenomenon was a common property of all species tested.</description><subject>Animals</subject><subject>Brain - enzymology</subject><subject>Circular Dichroism</subject><subject>Enzymes-esterases hydrolyzing oxazepam acetate in vivo and in vitro</subject><subject>Enzymes—esterases hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined</subject><subject>Esterases - metabolism</subject><subject>Esterases-hydrolyzing oxazepam acetate in vivo and in vitro</subject><subject>Esterases—hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined</subject><subject>hydrolysis of acetate ester in vivo and in vitro</subject><subject>Hydrolysis-oxazepam acetate in vivo and in vitro</subject><subject>Hydrolysis—oxazepam acetate in vivo and in vitro stereospecificity of esterases determined</subject><subject>In Vitro Techniques</subject><subject>Kinetics</subject><subject>Liver - enzymology</subject><subject>Male</subject><subject>Mice</subject><subject>Molecular Conformation</subject><subject>Oxazepam - analogs & derivatives</subject><subject>Oxazepam - metabolism</subject><subject>Oxazepam acetate-hydrolysis in vivo and in vitro</subject><subject>Oxazepam acetate—hydrolysis in vivo and in vitro stereospecificity of esterases determined</subject><subject>stereospecificity determined</subject><subject>stereospecificity of esterases determined</subject><subject>Stereospecificity-esterases hydrolyzing oxazepam acetate in vivo and in vitro</subject><subject>Subcellular Fractions - enzymology</subject><subject>Tranquilizers-oxazepam</subject><subject>Tranquilizers—oxazepam hydrolysis of acetate ester in vivo and in vitro, stereospecificity of esterases determined</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1978</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkElPwzAQRi3EVpYrJw45cUvxEiexOKGqlKWioII4Wo4zQYakCXYKpL8eoyAQB8RppJn3fdI8hA4IHhKM6fFT44Y0xjhOsMB8DQ0IpziMMUnW0cADNGQ8Ettox7kn7DHM-RbajAVOKRmgk3kLFmrXgDaF0abtgroIxs5vlQMXnHe5rctuZRaPwexdraBRVXCqoVUt7KGNQpUO9r_mLro_G9-NzsPpbHIxOp2GOhKUhyrNMs5ozhKhIKOK6kRhzfM0TphQItWC6JxnMSEa8oxBBASKKBWKZ8AgVWwXHfW9ja1fluBaWRmnoSzVAuqlk0lEIhFx5sFhD2pbO2ehkI01lbKdJFh-ypJelvyR5QOHX83LrIL8G-_t-LPoz2-mhO6fMnl5M_9VHfZZ412-f2eVfZb-74TLh-uJvLui5IbOb-XU82nPgzf5asBKpw0svBJjQbcyr81fX3wARFKYgg</recordid><startdate>197809</startdate><enddate>197809</enddate><creator>Maksay, Gabor</creator><creator>Tegyey, Zsuzsanna</creator><creator>Ötvös, László</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><scope>BSCLL</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>197809</creationdate><title>Stereospecificity of Esterases Hydrolyzing Oxazepam Acetate</title><author>Maksay, Gabor ; Tegyey, Zsuzsanna ; Ötvös, László</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4925-a8bb532d379aeb2a2c7a0c5d86739a98c91cd5b611cedb3e4e1ef489a5be3e8a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1978</creationdate><topic>Animals</topic><topic>Brain - enzymology</topic><topic>Circular Dichroism</topic><topic>Enzymes-esterases hydrolyzing oxazepam acetate in vivo and in vitro</topic><topic>Enzymes—esterases hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined</topic><topic>Esterases - metabolism</topic><topic>Esterases-hydrolyzing oxazepam acetate in vivo and in vitro</topic><topic>Esterases—hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined</topic><topic>hydrolysis of acetate ester in vivo and in vitro</topic><topic>Hydrolysis-oxazepam acetate in vivo and in vitro</topic><topic>Hydrolysis—oxazepam acetate in vivo and in vitro stereospecificity of esterases determined</topic><topic>In Vitro Techniques</topic><topic>Kinetics</topic><topic>Liver - enzymology</topic><topic>Male</topic><topic>Mice</topic><topic>Molecular Conformation</topic><topic>Oxazepam - analogs & derivatives</topic><topic>Oxazepam - metabolism</topic><topic>Oxazepam acetate-hydrolysis in vivo and in vitro</topic><topic>Oxazepam acetate—hydrolysis in vivo and in vitro stereospecificity of esterases determined</topic><topic>stereospecificity determined</topic><topic>stereospecificity of esterases determined</topic><topic>Stereospecificity-esterases hydrolyzing oxazepam acetate in vivo and in vitro</topic><topic>Subcellular Fractions - enzymology</topic><topic>Tranquilizers-oxazepam</topic><topic>Tranquilizers—oxazepam hydrolysis of acetate ester in vivo and in vitro, stereospecificity of esterases determined</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Maksay, Gabor</creatorcontrib><creatorcontrib>Tegyey, Zsuzsanna</creatorcontrib><creatorcontrib>Ötvös, László</creatorcontrib><collection>Istex</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>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Maksay, Gabor</au><au>Tegyey, Zsuzsanna</au><au>Ötvös, László</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Stereospecificity of Esterases Hydrolyzing Oxazepam Acetate</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>1978-09</date><risdate>1978</risdate><volume>67</volume><issue>9</issue><spage>1208</spage><epage>1210</epage><pages>1208-1210</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><abstract>Esterases hydrolyzing the racemic acetate ester of the centrally acting drug oxazepam in mice were examined. Radiolabeled ester administered intravenously was hydrolyzed rapidly in the liver, kidneys, and brain. The distribution of the enzyme activity of liver and brain subcellular fractions was measured. Kinetic data and structure investigation of partially hydrolyzed racemic ester pointed to the stereoselectivity of liver and brain esterases. The preferred hydrolysis of the (R)-(−)-isomer in liver homogenates was attributed mainly to microsomal enzymes, while that of the (S)-(+)-isomer in brain was considered to be due to the mitochondrial fraction. This phenomenon was a common property of all species tested.</abstract><cop>Washington</cop><pub>Elsevier Inc</pub><pmid>690821</pmid><doi>10.1002/jps.2600670905</doi><tpages>3</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0022-3549 |
| ispartof | Journal of pharmaceutical sciences, 1978-09, Vol.67 (9), p.1208-1210 |
| issn | 0022-3549 1520-6017 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_74149453 |
| source | MEDLINE; Wiley Online Library Journals Frontfile Complete; Alma/SFX Local Collection |
| subjects | Animals Brain - enzymology Circular Dichroism Enzymes-esterases hydrolyzing oxazepam acetate in vivo and in vitro Enzymes—esterases hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined Esterases - metabolism Esterases-hydrolyzing oxazepam acetate in vivo and in vitro Esterases—hydrolyzing oxazepam acetate in vivo and in vitro stereospecificity determined hydrolysis of acetate ester in vivo and in vitro Hydrolysis-oxazepam acetate in vivo and in vitro Hydrolysis—oxazepam acetate in vivo and in vitro stereospecificity of esterases determined In Vitro Techniques Kinetics Liver - enzymology Male Mice Molecular Conformation Oxazepam - analogs & derivatives Oxazepam - metabolism Oxazepam acetate-hydrolysis in vivo and in vitro Oxazepam acetate—hydrolysis in vivo and in vitro stereospecificity of esterases determined stereospecificity determined stereospecificity of esterases determined Stereospecificity-esterases hydrolyzing oxazepam acetate in vivo and in vitro Subcellular Fractions - enzymology Tranquilizers-oxazepam Tranquilizers—oxazepam hydrolysis of acetate ester in vivo and in vitro, stereospecificity of esterases determined |
| title | Stereospecificity of Esterases Hydrolyzing Oxazepam Acetate |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-04T11%3A52%3A45IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Stereospecificity%20of%20Esterases%20Hydrolyzing%20Oxazepam%20Acetate&rft.jtitle=Journal%20of%20pharmaceutical%20sciences&rft.au=Maksay,%20Gabor&rft.date=1978-09&rft.volume=67&rft.issue=9&rft.spage=1208&rft.epage=1210&rft.pages=1208-1210&rft.issn=0022-3549&rft.eissn=1520-6017&rft_id=info:doi/10.1002/jps.2600670905&rft_dat=%3Cproquest_cross%3E74149453%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=74149453&rft_id=info:pmid/690821&rft_els_id=S0022354915422300&rfr_iscdi=true |