Involvement of P-glycoprotein in Blood–Brain Barrier Transport of Pentazocine in Rats Using Brain Uptake Index Method
The involvement of P-glycoprotein (P-gp) in pentazocine (PTZ) transport at the blood–brain barrier (BBB) in rats was evaluated by means of an in vivo study using the brain uptake index (BUI) method. The amount of radioactivity in the brain was estimated at different intervals (up to 240 s) after car...
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| Veröffentlicht in: | Biological & pharmaceutical bulletin 2004, Vol.27(6), pp.932-935 |
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| creator | Moriki, Yoshiaki Suzuki, Toyofumi Fukami, Toshiro Hanano, Manabu Tomono, Kazuo Watanabe, Jun |
| description | The involvement of P-glycoprotein (P-gp) in pentazocine (PTZ) transport at the blood–brain barrier (BBB) in rats was evaluated by means of an in vivo study using the brain uptake index (BUI) method. The amount of radioactivity in the brain was estimated at different intervals (up to 240 s) after carotid injection in rats. The apparent elimination rate constant (ktest) due to efflux of PTZ from the brain was calculated as 0.22 min−1. The observed BUI values of [3H]-PTZ (0.35 μM) were not significantly different between 5 and 15 s after the carotid injection. The concentration-dependent uptake of PTZ by the brain was increased gradually by increasing the concentration (0.01—1 mM) of PTZ in the injection solution. The apparent uptake of PTZ by the brain increased in the presence of P-gp inhibitors such as cyclosporin A, quinidine, verapamil and vinblastine after the carotid injection. These results suggest that the increment of PTZ uptake by the brain could be explained by the saturable efflux transport system involving a P-gp-mediated efflux mechanism of PTZ transport at the BBB. |
| doi_str_mv | 10.1248/bpb.27.932 |
| format | Article |
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The amount of radioactivity in the brain was estimated at different intervals (up to 240 s) after carotid injection in rats. The apparent elimination rate constant (ktest) due to efflux of PTZ from the brain was calculated as 0.22 min−1. The observed BUI values of [3H]-PTZ (0.35 μM) were not significantly different between 5 and 15 s after the carotid injection. The concentration-dependent uptake of PTZ by the brain was increased gradually by increasing the concentration (0.01—1 mM) of PTZ in the injection solution. The apparent uptake of PTZ by the brain increased in the presence of P-gp inhibitors such as cyclosporin A, quinidine, verapamil and vinblastine after the carotid injection. These results suggest that the increment of PTZ uptake by the brain could be explained by the saturable efflux transport system involving a P-gp-mediated efflux mechanism of PTZ transport at the BBB.</description><identifier>ISSN: 0918-6158</identifier><identifier>EISSN: 1347-5215</identifier><identifier>DOI: 10.1248/bpb.27.932</identifier><identifier>PMID: 15187451</identifier><language>eng</language><publisher>Japan: The Pharmaceutical Society of Japan</publisher><subject>Animals ; ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism ; Biological Transport - physiology ; Blood-Brain Barrier - metabolism ; blood–brain barrier ; Brain - metabolism ; brain uptake index ; efflux transport ; Female ; P-glycoprotein ; pentazocine ; Pentazocine - metabolism ; Rats ; Rats, Wistar</subject><ispartof>Biological and Pharmaceutical Bulletin, 2004, Vol.27(6), pp.932-935</ispartof><rights>2004 The Pharmaceutical Society of Japan</rights><rights>Copyright Japan Science and Technology Agency 2004</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c552t-94c022a004bf9087aaeb7a6db4c4e53ad9c9393ea772acc776b366a5f97e0eb83</citedby><cites>FETCH-LOGICAL-c552t-94c022a004bf9087aaeb7a6db4c4e53ad9c9393ea772acc776b366a5f97e0eb83</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,781,785,1884,27925,27926</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15187451$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Moriki, Yoshiaki</creatorcontrib><creatorcontrib>Suzuki, Toyofumi</creatorcontrib><creatorcontrib>Fukami, Toshiro</creatorcontrib><creatorcontrib>Hanano, Manabu</creatorcontrib><creatorcontrib>Tomono, Kazuo</creatorcontrib><creatorcontrib>Watanabe, Jun</creatorcontrib><title>Involvement of P-glycoprotein in Blood–Brain Barrier Transport of Pentazocine in Rats Using Brain Uptake Index Method</title><title>Biological & pharmaceutical bulletin</title><addtitle>Biol Pharm Bull</addtitle><description>The involvement of P-glycoprotein (P-gp) in pentazocine (PTZ) transport at the blood–brain barrier (BBB) in rats was evaluated by means of an in vivo study using the brain uptake index (BUI) method. The amount of radioactivity in the brain was estimated at different intervals (up to 240 s) after carotid injection in rats. The apparent elimination rate constant (ktest) due to efflux of PTZ from the brain was calculated as 0.22 min−1. The observed BUI values of [3H]-PTZ (0.35 μM) were not significantly different between 5 and 15 s after the carotid injection. The concentration-dependent uptake of PTZ by the brain was increased gradually by increasing the concentration (0.01—1 mM) of PTZ in the injection solution. The apparent uptake of PTZ by the brain increased in the presence of P-gp inhibitors such as cyclosporin A, quinidine, verapamil and vinblastine after the carotid injection. These results suggest that the increment of PTZ uptake by the brain could be explained by the saturable efflux transport system involving a P-gp-mediated efflux mechanism of PTZ transport at the BBB.</description><subject>Animals</subject><subject>ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism</subject><subject>Biological Transport - physiology</subject><subject>Blood-Brain Barrier - metabolism</subject><subject>blood–brain barrier</subject><subject>Brain - metabolism</subject><subject>brain uptake index</subject><subject>efflux transport</subject><subject>Female</subject><subject>P-glycoprotein</subject><subject>pentazocine</subject><subject>Pentazocine - metabolism</subject><subject>Rats</subject><subject>Rats, Wistar</subject><issn>0918-6158</issn><issn>1347-5215</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkd2KFDEQhYMo7rh64wNIg-CF0GN-O91X4i7-DKwosnMdqtPVsz32JL1JZnW98h18Q5_EDD2uIBQpinznUMkh5CmjS8Zl_aqd2iXXy0bwe2TBhNSl4kzdJwvasLqsmKpPyKMYt5RSTbl4SE6YYrWWii3It5W78eMN7tClwvfF53Iz3lo_BZ9wcEWus9H77vfPX2cBDhOEMGAoLgO4OPkwi7IYfng7ODwovkCKxToOblPMovWU4CsWK9fh9-IjpivfPSYPehgjPjn2U7J-9_by_EN58en96vzNRWmV4qlspKWcA6Wy7RtaawBsNVRdK61EJaBrbCMagaA1B2u1rlpRVaD6RiPFthan5MXsm190vceYzG6IFscRHPp9NJpTKmSlM_j8P3Dr98Hl3QyTshGiUuJAvZwpG3yMAXszhWEH4dYwag5hmByG4drkMDL87Gi5b3fY_UOPv5-B1zOwjQk2eAdASIMd8a9XNR_Z8u7GXkEw6MQf7aydkQ</recordid><startdate>20040601</startdate><enddate>20040601</enddate><creator>Moriki, Yoshiaki</creator><creator>Suzuki, Toyofumi</creator><creator>Fukami, Toshiro</creator><creator>Hanano, Manabu</creator><creator>Tomono, Kazuo</creator><creator>Watanabe, Jun</creator><general>The Pharmaceutical Society of Japan</general><general>Japan Science and Technology Agency</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>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U9</scope><scope>8FD</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20040601</creationdate><title>Involvement of P-glycoprotein in Blood–Brain Barrier Transport of Pentazocine in Rats Using Brain Uptake Index Method</title><author>Moriki, Yoshiaki ; Suzuki, Toyofumi ; Fukami, Toshiro ; Hanano, Manabu ; Tomono, Kazuo ; Watanabe, Jun</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c552t-94c022a004bf9087aaeb7a6db4c4e53ad9c9393ea772acc776b366a5f97e0eb83</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Animals</topic><topic>ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism</topic><topic>Biological Transport - physiology</topic><topic>Blood-Brain Barrier - metabolism</topic><topic>blood–brain barrier</topic><topic>Brain - metabolism</topic><topic>brain uptake index</topic><topic>efflux transport</topic><topic>Female</topic><topic>P-glycoprotein</topic><topic>pentazocine</topic><topic>Pentazocine - metabolism</topic><topic>Rats</topic><topic>Rats, Wistar</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Moriki, Yoshiaki</creatorcontrib><creatorcontrib>Suzuki, Toyofumi</creatorcontrib><creatorcontrib>Fukami, Toshiro</creatorcontrib><creatorcontrib>Hanano, Manabu</creatorcontrib><creatorcontrib>Tomono, Kazuo</creatorcontrib><creatorcontrib>Watanabe, Jun</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Biological & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Moriki, Yoshiaki</au><au>Suzuki, Toyofumi</au><au>Fukami, Toshiro</au><au>Hanano, Manabu</au><au>Tomono, Kazuo</au><au>Watanabe, Jun</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Involvement of P-glycoprotein in Blood–Brain Barrier Transport of Pentazocine in Rats Using Brain Uptake Index Method</atitle><jtitle>Biological & pharmaceutical bulletin</jtitle><addtitle>Biol Pharm Bull</addtitle><date>2004-06-01</date><risdate>2004</risdate><volume>27</volume><issue>6</issue><spage>932</spage><epage>935</epage><pages>932-935</pages><issn>0918-6158</issn><eissn>1347-5215</eissn><abstract>The involvement of P-glycoprotein (P-gp) in pentazocine (PTZ) transport at the blood–brain barrier (BBB) in rats was evaluated by means of an in vivo study using the brain uptake index (BUI) method. The amount of radioactivity in the brain was estimated at different intervals (up to 240 s) after carotid injection in rats. The apparent elimination rate constant (ktest) due to efflux of PTZ from the brain was calculated as 0.22 min−1. The observed BUI values of [3H]-PTZ (0.35 μM) were not significantly different between 5 and 15 s after the carotid injection. The concentration-dependent uptake of PTZ by the brain was increased gradually by increasing the concentration (0.01—1 mM) of PTZ in the injection solution. The apparent uptake of PTZ by the brain increased in the presence of P-gp inhibitors such as cyclosporin A, quinidine, verapamil and vinblastine after the carotid injection. 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| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Animals ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism Biological Transport - physiology Blood-Brain Barrier - metabolism blood–brain barrier Brain - metabolism brain uptake index efflux transport Female P-glycoprotein pentazocine Pentazocine - metabolism Rats Rats, Wistar |
| title | Involvement of P-glycoprotein in Blood–Brain Barrier Transport of Pentazocine in Rats Using Brain Uptake Index Method |
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