Characteristic glucuronidation pattern of physiologic concentration of morphine in rat brain
Formation of conjugated metabolites from morphine at a very low level in brain was studied in vitro in rats. Incubation of a low concentration of 3H-morphine with brain homogenate followed by two successive high-performance liquid chromatographic analyses showed that endogenous morphine is converted...
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| Veröffentlicht in: | Life sciences (1973) 2000-10, Vol.67 (20), p.2453-2464 |
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| container_title | Life sciences (1973) |
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| creator | Nagano, Emiko Yamada, Hideyuki Oguri, Kazuta |
| description | Formation of conjugated metabolites from morphine at a very low level in brain was studied in vitro in rats. Incubation of a low concentration of
3H-morphine with brain homogenate followed by two successive high-performance liquid chromatographic analyses showed that endogenous morphine is converted by brain enzymes to its 3- and 6-glucuronides (M-3-G and M-6-G), and codeine glucuronide (Cod-G). However, the formation of morphine-6-sulfate was likely to be low if it was produced at all. All of the cerebral hemisphere, brain stem and cerebellum were capable of producing M-3-G, M-6-G and Cod-G, although there were differences in selectivity. The capacity of the brain for glucuronide formation was far less than that of the liver, but UDP-glucuronosyltransferase in brain was much more selective in forming M-6-G and Cod-G than liver enzymes. |
| doi_str_mv | 10.1016/S0024-3205(00)00825-0 |
| format | Article |
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3H-morphine with brain homogenate followed by two successive high-performance liquid chromatographic analyses showed that endogenous morphine is converted by brain enzymes to its 3- and 6-glucuronides (M-3-G and M-6-G), and codeine glucuronide (Cod-G). However, the formation of morphine-6-sulfate was likely to be low if it was produced at all. All of the cerebral hemisphere, brain stem and cerebellum were capable of producing M-3-G, M-6-G and Cod-G, although there were differences in selectivity. The capacity of the brain for glucuronide formation was far less than that of the liver, but UDP-glucuronosyltransferase in brain was much more selective in forming M-6-G and Cod-G than liver enzymes.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/S0024-3205(00)00825-0</identifier><identifier>PMID: 11065168</identifier><language>eng</language><publisher>Netherlands: Elsevier Inc</publisher><subject>Animals ; Brain ; Brain - enzymology ; Brain Stem - metabolism ; Cerebellum - metabolism ; Chromatography, High Pressure Liquid ; Codeine - analogs & derivatives ; Codeine - metabolism ; Codeine glucuronide ; Endogenous morphine ; Glucuronides - metabolism ; Glucuronosyltransferase - metabolism ; Liver - metabolism ; Male ; Microsomes, Liver - enzymology ; Microsomes, Liver - metabolism ; Morphine - metabolism ; Morphine Derivatives - metabolism ; Morphine-3-glucuronide ; Morphine-6-glucuronide ; Rat ; Rats ; Rats, Sprague-Dawley ; Telencephalon - metabolism ; UDP-Glucuronosyltransferase</subject><ispartof>Life sciences (1973), 2000-10, Vol.67 (20), p.2453-2464</ispartof><rights>2000 Elsevier Science Inc.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c479t-d1dacae2be6a8bfd84460c51177e1c6e0fd641256c0e275ffe9257b5f5980b703</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0024-3205(00)00825-0$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,782,786,3552,27931,27932,46002</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11065168$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nagano, Emiko</creatorcontrib><creatorcontrib>Yamada, Hideyuki</creatorcontrib><creatorcontrib>Oguri, Kazuta</creatorcontrib><title>Characteristic glucuronidation pattern of physiologic concentration of morphine in rat brain</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>Formation of conjugated metabolites from morphine at a very low level in brain was studied in vitro in rats. Incubation of a low concentration of
3H-morphine with brain homogenate followed by two successive high-performance liquid chromatographic analyses showed that endogenous morphine is converted by brain enzymes to its 3- and 6-glucuronides (M-3-G and M-6-G), and codeine glucuronide (Cod-G). However, the formation of morphine-6-sulfate was likely to be low if it was produced at all. All of the cerebral hemisphere, brain stem and cerebellum were capable of producing M-3-G, M-6-G and Cod-G, although there were differences in selectivity. The capacity of the brain for glucuronide formation was far less than that of the liver, but UDP-glucuronosyltransferase in brain was much more selective in forming M-6-G and Cod-G than liver enzymes.</description><subject>Animals</subject><subject>Brain</subject><subject>Brain - enzymology</subject><subject>Brain Stem - metabolism</subject><subject>Cerebellum - metabolism</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Codeine - analogs & derivatives</subject><subject>Codeine - metabolism</subject><subject>Codeine glucuronide</subject><subject>Endogenous morphine</subject><subject>Glucuronides - metabolism</subject><subject>Glucuronosyltransferase - metabolism</subject><subject>Liver - metabolism</subject><subject>Male</subject><subject>Microsomes, Liver - enzymology</subject><subject>Microsomes, Liver - metabolism</subject><subject>Morphine - metabolism</subject><subject>Morphine Derivatives - metabolism</subject><subject>Morphine-3-glucuronide</subject><subject>Morphine-6-glucuronide</subject><subject>Rat</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Telencephalon - metabolism</subject><subject>UDP-Glucuronosyltransferase</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1LxDAQhoMo7vrxE5SeRA_VSdsk7Ulk8QsWPKg3IaTpdDfSTWrSCvvv7W4XPXoamHlmXuYh5IzCNQXKb14BkixOE2CXAFcAecJi2CNTmosiBp7SfTL9RSbkKIRPAGBMpIdkQilwRnk-JR-zpfJKd-hN6IyOFk2ve--sqVRnnI1a1Q0zG7k6apfrYFzjFgOmndVoOz9Cw3DlfLs0FiNjo6EblV4Ze0IOatUEPN3VY_L-cP82e4rnL4_Ps7t5rDNRdHFFK6UVJiVylZd1lWcZB80oFQKp5gh1xTOaMK4BE8HqGouEiZLVrMihFJAek4vxbuvdV4-hkysTNDaNsuj6IEWS5qzgYgDZCGrvQvBYy9ablfJrSUFutMqtVrlxJgHkVqvcBJzvAvpyhdXf1s7jANyOAA5vfhv0MmiDg6PKeNSdrJz5J-IH24CJFA</recordid><startdate>20001006</startdate><enddate>20001006</enddate><creator>Nagano, Emiko</creator><creator>Yamada, Hideyuki</creator><creator>Oguri, Kazuta</creator><general>Elsevier Inc</general><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>20001006</creationdate><title>Characteristic glucuronidation pattern of physiologic concentration of morphine in rat brain</title><author>Nagano, Emiko ; Yamada, Hideyuki ; Oguri, Kazuta</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c479t-d1dacae2be6a8bfd84460c51177e1c6e0fd641256c0e275ffe9257b5f5980b703</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Animals</topic><topic>Brain</topic><topic>Brain - enzymology</topic><topic>Brain Stem - metabolism</topic><topic>Cerebellum - metabolism</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Codeine - analogs & derivatives</topic><topic>Codeine - metabolism</topic><topic>Codeine glucuronide</topic><topic>Endogenous morphine</topic><topic>Glucuronides - metabolism</topic><topic>Glucuronosyltransferase - metabolism</topic><topic>Liver - metabolism</topic><topic>Male</topic><topic>Microsomes, Liver - enzymology</topic><topic>Microsomes, Liver - metabolism</topic><topic>Morphine - metabolism</topic><topic>Morphine Derivatives - metabolism</topic><topic>Morphine-3-glucuronide</topic><topic>Morphine-6-glucuronide</topic><topic>Rat</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Telencephalon - metabolism</topic><topic>UDP-Glucuronosyltransferase</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nagano, Emiko</creatorcontrib><creatorcontrib>Yamada, Hideyuki</creatorcontrib><creatorcontrib>Oguri, Kazuta</creatorcontrib><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>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nagano, Emiko</au><au>Yamada, Hideyuki</au><au>Oguri, Kazuta</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Characteristic glucuronidation pattern of physiologic concentration of morphine in rat brain</atitle><jtitle>Life sciences (1973)</jtitle><addtitle>Life Sci</addtitle><date>2000-10-06</date><risdate>2000</risdate><volume>67</volume><issue>20</issue><spage>2453</spage><epage>2464</epage><pages>2453-2464</pages><issn>0024-3205</issn><eissn>1879-0631</eissn><abstract>Formation of conjugated metabolites from morphine at a very low level in brain was studied in vitro in rats. Incubation of a low concentration of
3H-morphine with brain homogenate followed by two successive high-performance liquid chromatographic analyses showed that endogenous morphine is converted by brain enzymes to its 3- and 6-glucuronides (M-3-G and M-6-G), and codeine glucuronide (Cod-G). However, the formation of morphine-6-sulfate was likely to be low if it was produced at all. All of the cerebral hemisphere, brain stem and cerebellum were capable of producing M-3-G, M-6-G and Cod-G, although there were differences in selectivity. The capacity of the brain for glucuronide formation was far less than that of the liver, but UDP-glucuronosyltransferase in brain was much more selective in forming M-6-G and Cod-G than liver enzymes.</abstract><cop>Netherlands</cop><pub>Elsevier Inc</pub><pmid>11065168</pmid><doi>10.1016/S0024-3205(00)00825-0</doi><tpages>12</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0024-3205 |
| ispartof | Life sciences (1973), 2000-10, Vol.67 (20), p.2453-2464 |
| issn | 0024-3205 1879-0631 |
| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals Brain Brain - enzymology Brain Stem - metabolism Cerebellum - metabolism Chromatography, High Pressure Liquid Codeine - analogs & derivatives Codeine - metabolism Codeine glucuronide Endogenous morphine Glucuronides - metabolism Glucuronosyltransferase - metabolism Liver - metabolism Male Microsomes, Liver - enzymology Microsomes, Liver - metabolism Morphine - metabolism Morphine Derivatives - metabolism Morphine-3-glucuronide Morphine-6-glucuronide Rat Rats Rats, Sprague-Dawley Telencephalon - metabolism UDP-Glucuronosyltransferase |
| title | Characteristic glucuronidation pattern of physiologic concentration of morphine in rat brain |
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