Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site
Two phencyclidine (PCP) analogs, 3 and 4, and one thienylcyclohexyl‐piperidine (TCP) analog, (±)6, were labeled with positron emitter carbon‐11. These compounds displayed higher in vitro binding affinities than PCP itself for the PCP‐binding site located inside the ion channel on the N‐methyl‐D‐aspa...
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| Veröffentlicht in: | Journal of labelled compounds & radiopharmaceuticals 1998-09, Vol.41 (9), p.843-858 |
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| container_title | Journal of labelled compounds & radiopharmaceuticals |
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| creator | Haradahira, Terushi Sasaki, Sigeki Maeda, Minoru Kobayashi, Kaoru Inoue, Osamu Tomita, Urara Nishikawa, Toru Suzuki, Kazutoshi |
| description | Two phencyclidine (PCP) analogs, 3 and 4, and one thienylcyclohexyl‐piperidine (TCP) analog, (±)6, were labeled with positron emitter carbon‐11. These compounds displayed higher in vitro binding affinities than PCP itself for the PCP‐binding site located inside the ion channel on the N‐methyl‐D‐aspartate (NMDA) receptors. Brain distribution studies in mice showed different uptake characteristics between the PCP and TCP analogs, indicating their different in vivo interactions with the brain components including the PCP‐binding site probably due to the different physicochemical properties of the molecules. © 1998 John Wiley & Sons, Ltd. |
| doi_str_mv | 10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H |
| format | Article |
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These compounds displayed higher in vitro binding affinities than PCP itself for the PCP‐binding site located inside the ion channel on the N‐methyl‐D‐aspartate (NMDA) receptors. Brain distribution studies in mice showed different uptake characteristics between the PCP and TCP analogs, indicating their different in vivo interactions with the brain components including the PCP‐binding site probably due to the different physicochemical properties of the molecules. © 1998 John Wiley & Sons, Ltd.</description><identifier>ISSN: 0362-4803</identifier><identifier>EISSN: 1099-1344</identifier><identifier>DOI: 10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H</identifier><language>eng</language><publisher>Chichester: John Wiley & Sons, Ltd</publisher><subject>Biological and medical sciences ; carbon-11 ; Contrast media. Radiopharmaceuticals ; Glutamatergic system (aspartate and other excitatory aminoacids) ; Medical sciences ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; NMDA receptor ; Pharmacology. Drug treatments ; phencyclidine ; positron emission tomography ; thienylcyclohexylpiperidine</subject><ispartof>Journal of labelled compounds & radiopharmaceuticals, 1998-09, Vol.41 (9), p.843-858</ispartof><rights>Copyright © 1998 John Wiley & Sons, Ltd.</rights><rights>1998 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c4166-6de65d856f0406d092e5bfc11cfd99f20574e132df4d0058ba02dc734f3e1b7d3</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%2F%28SICI%291099-1344%281998090%2941%3A9%3C843%3A%3AAID-JLCR136%3E3.0.CO%3B2-H$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2F%28SICI%291099-1344%281998090%2941%3A9%3C843%3A%3AAID-JLCR136%3E3.0.CO%3B2-H$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2374441$$DView record in Pascal Francis$$Hfree_for_read</backlink></links><search><creatorcontrib>Haradahira, Terushi</creatorcontrib><creatorcontrib>Sasaki, Sigeki</creatorcontrib><creatorcontrib>Maeda, Minoru</creatorcontrib><creatorcontrib>Kobayashi, Kaoru</creatorcontrib><creatorcontrib>Inoue, Osamu</creatorcontrib><creatorcontrib>Tomita, Urara</creatorcontrib><creatorcontrib>Nishikawa, Toru</creatorcontrib><creatorcontrib>Suzuki, Kazutoshi</creatorcontrib><title>Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site</title><title>Journal of labelled compounds & radiopharmaceuticals</title><addtitle>J Label Compd Radiopharm</addtitle><description>Two phencyclidine (PCP) analogs, 3 and 4, and one thienylcyclohexyl‐piperidine (TCP) analog, (±)6, were labeled with positron emitter carbon‐11. These compounds displayed higher in vitro binding affinities than PCP itself for the PCP‐binding site located inside the ion channel on the N‐methyl‐D‐aspartate (NMDA) receptors. Brain distribution studies in mice showed different uptake characteristics between the PCP and TCP analogs, indicating their different in vivo interactions with the brain components including the PCP‐binding site probably due to the different physicochemical properties of the molecules. © 1998 John Wiley & Sons, Ltd.</description><subject>Biological and medical sciences</subject><subject>carbon-11</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>Glutamatergic system (aspartate and other excitatory aminoacids)</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>NMDA receptor</subject><subject>Pharmacology. Drug treatments</subject><subject>phencyclidine</subject><subject>positron emission tomography</subject><subject>thienylcyclohexylpiperidine</subject><issn>0362-4803</issn><issn>1099-1344</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1998</creationdate><recordtype>article</recordtype><recordid>eNqFkU1vEzEQhlcIJELhP_iAUHvYYK-9Hw4IEW1pExSaQkBFcBh5_REMW2-wN4KIP49XCbmAxMnSzDvPWPMkyUuCxwTj7Onpal7PzwjmPCWUsVPCeYU5PmNkwp9XjE4m0_l5-npRvyO0eEHHeFwvn2Xp7E4yOg7dTUaYFlnKKkzvJw9C-Ipx7DE2Sn6tdq7_ooMNSDiFGi-sQ8qG3ttm29vOoc4gKXzTuZQQ1IpGt1rFrGi7dRiawvVi3bk4EpDpPIo0dPXmfIq8lnrTx4rstpth6Lq-ThvrlHVrFGyvHyb3jGiDfnR4T5IPF6_e17N0sbyc19NFKhkpirRQushVlRcGM1wozDOdN0YSIo3i3GQ4L5kmNFOGKYzzqhE4U7KkzFBNmlLRk-TJnrvx3fetDj3c2iB12wqnu20AUkYGISwGP-6D0ncheG1g4-2t8DsgGAYbAIMNGA4Lw2HhYAMYAQ7RBkC0AQcbQAFDvYQMZhH9-PAHEaRojRdO2nDkZ7RkjJEY-7yP_bCt3v21_n_b_738TynS0z09ytI_j3Thv0FR0jKHm6tLuJh9uslXbzPg9Dc6xLsc</recordid><startdate>199809</startdate><enddate>199809</enddate><creator>Haradahira, Terushi</creator><creator>Sasaki, Sigeki</creator><creator>Maeda, Minoru</creator><creator>Kobayashi, Kaoru</creator><creator>Inoue, Osamu</creator><creator>Tomita, Urara</creator><creator>Nishikawa, Toru</creator><creator>Suzuki, Kazutoshi</creator><general>John Wiley & Sons, Ltd</general><general>Wiley</general><scope>BSCLL</scope><scope>IQODW</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7TK</scope></search><sort><creationdate>199809</creationdate><title>Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site</title><author>Haradahira, Terushi ; Sasaki, Sigeki ; Maeda, Minoru ; Kobayashi, Kaoru ; Inoue, Osamu ; Tomita, Urara ; Nishikawa, Toru ; Suzuki, Kazutoshi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4166-6de65d856f0406d092e5bfc11cfd99f20574e132df4d0058ba02dc734f3e1b7d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1998</creationdate><topic>Biological and medical sciences</topic><topic>carbon-11</topic><topic>Contrast media. Radiopharmaceuticals</topic><topic>Glutamatergic system (aspartate and other excitatory aminoacids)</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>NMDA receptor</topic><topic>Pharmacology. Drug treatments</topic><topic>phencyclidine</topic><topic>positron emission tomography</topic><topic>thienylcyclohexylpiperidine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Haradahira, Terushi</creatorcontrib><creatorcontrib>Sasaki, Sigeki</creatorcontrib><creatorcontrib>Maeda, Minoru</creatorcontrib><creatorcontrib>Kobayashi, Kaoru</creatorcontrib><creatorcontrib>Inoue, Osamu</creatorcontrib><creatorcontrib>Tomita, Urara</creatorcontrib><creatorcontrib>Nishikawa, Toru</creatorcontrib><creatorcontrib>Suzuki, Kazutoshi</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Haradahira, Terushi</au><au>Sasaki, Sigeki</au><au>Maeda, Minoru</au><au>Kobayashi, Kaoru</au><au>Inoue, Osamu</au><au>Tomita, Urara</au><au>Nishikawa, Toru</au><au>Suzuki, Kazutoshi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site</atitle><jtitle>Journal of labelled compounds & radiopharmaceuticals</jtitle><addtitle>J Label Compd Radiopharm</addtitle><date>1998-09</date><risdate>1998</risdate><volume>41</volume><issue>9</issue><spage>843</spage><epage>858</epage><pages>843-858</pages><issn>0362-4803</issn><eissn>1099-1344</eissn><abstract>Two phencyclidine (PCP) analogs, 3 and 4, and one thienylcyclohexyl‐piperidine (TCP) analog, (±)6, were labeled with positron emitter carbon‐11. These compounds displayed higher in vitro binding affinities than PCP itself for the PCP‐binding site located inside the ion channel on the N‐methyl‐D‐aspartate (NMDA) receptors. Brain distribution studies in mice showed different uptake characteristics between the PCP and TCP analogs, indicating their different in vivo interactions with the brain components including the PCP‐binding site probably due to the different physicochemical properties of the molecules. © 1998 John Wiley & Sons, Ltd.</abstract><cop>Chichester</cop><pub>John Wiley & Sons, Ltd</pub><doi>10.1002/(SICI)1099-1344(1998090)41:9<843::AID-JLCR136>3.0.CO;2-H</doi><tpages>16</tpages></addata></record> |
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| identifier | ISSN: 0362-4803 |
| ispartof | Journal of labelled compounds & radiopharmaceuticals, 1998-09, Vol.41 (9), p.843-858 |
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| language | eng |
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| source | Wiley Journals |
| subjects | Biological and medical sciences carbon-11 Contrast media. Radiopharmaceuticals Glutamatergic system (aspartate and other excitatory aminoacids) Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors NMDA receptor Pharmacology. Drug treatments phencyclidine positron emission tomography thienylcyclohexylpiperidine |
| title | Synthesis and brain distribution of carbon-11 labeled analogs of antagonists for the NMDA receptor coupled PCP-binding site |
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