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Synthesis,in vitro and in vivo pharmacology of a C-11 labeled analog of CP-101,606,(+/-)threo-1-(4-hydroxyphenyl)-2-[4-hydroxy-4-(p-[11C]methoxyphenyl)piperidino]-1-propanol,as a PET tracer for NR2B subunit-containing NMDA receptors
https://repo.qst.go.jp/records/44313
https://repo.qst.go.jp/records/44313cc903be5-f6e7-4c2e-95cf-68507a14adcb
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-21 | |||||
| タイトル | ||||||
| タイトル | Synthesis,in vitro and in vivo pharmacology of a C-11 labeled analog of CP-101,606,(+/-)threo-1-(4-hydroxyphenyl)-2-[4-hydroxy-4-(p-[11C]methoxyphenyl)piperidino]-1-propanol,as a PET tracer for NR2B subunit-containing NMDA receptors | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Haradahira, Terushi
× Haradahira, Terushi× Maeda, Jun× Okauchi, Takashi× Zhang, Ming-Rong× Hojo, Junko× Kida, Takayo× Arai, Takuya× Yamamoto, Fumihiko× Sasaki, Shigeki× Maeda, Minoru× Suzuki, Kazutoshi× Suhara, Tetsuya× 原田平 輝志× 前田 純× 岡内 隆× 張 明栄× 荒井 拓也× 佐々木 茂貴× 前田 稔× 鈴木 和年× 須原 哲也 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | A carbon-11 labeled methoxyl analog of CP-101,606,(+/-)threo-1-(4-hydroxyphenyl)-2-[4-hydroxy-4-(p-[11C]methoxyphenyl)piper-idino]-1-propanol[(+/-)[11C]1],was synthesized as a new subtype-selective PET radioligand for NMDA receptors.The in vitro binding studies using rat brain slices demonstrated that (+/-)[11C]1 shows an extremely high-specific binding to the NR2B subunit of NMDA receptors. In contrast to the in vitro binding,the in vivo binding to mouse and monkey brains showed no apparent specific localization of the radioactivity in any of the brain regions. Metabolism and physicochemical properties such as the lipophilicity of (+/-)[11C]1 seemed unlikely to affect the in vivo (+/-)[11C]1 binding. Among the various endogenous ligands acting at the NMDA receptors,polyamines(spermine and spermidine)and divalent cations(Mg2+.Zn2+.and Ca2+)strongly inhibited the in vitro(+/-)[11C]1 binding. Thus,the present studies point to the possibility that the polyamines and cations behave as endogenous inhibitors for (+/-)[11C]1 binding,leading to the loss of the specific binding in vivo. | |||||
| 書誌情報 |
Nuclear Medicine and Biology 巻 29, p. 517-525, 発行日 2002-10 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0969-8051 | |||||
