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Effects of Endogenous Agonists, Glycine and D-Serine, on In Vivo Specific Binding of [11C]L-703,717, a PET Radioligand for the Glycine-Binding Site of NMDA Receptors
https://repo.qst.go.jp/records/44327
https://repo.qst.go.jp/records/44327adfcbd64-94b9-4bb7-b77a-622e6153a8d6
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-23 | |||||
| タイトル | ||||||
| タイトル | Effects of Endogenous Agonists, Glycine and D-Serine, on In Vivo Specific Binding of [11C]L-703,717, a PET Radioligand for the Glycine-Binding Site of 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× Okauchi, Takashi× Maeda, Jun× Zhang, Ming-Rong× Nishikawa, Touru× Suzuki, Kazutoshi× Suhara, Tetsuya× 原田平 輝志× 岡内 隆× 前田 純× 張 明栄× 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 positron-emitter (carbon-11) labeled antagonist for the glycine-binding site of NMDA receptors, [11C]L-703,717, has a unique in vivo binding characteristic, in which it preferentially binds to cerebellar-specific NMDA receptors consisting of GluRe3 subunit and eventually accumulates in rodent cerebellum under in vivo conditions, but not under in vitro conditions. In order to understand the in vivo-specific site and subunit localization of this radioligand, we examined the effect of endogenous glycine site agonists, glycine and D-serine, on in vivo [11C]L-703,717 binding. An increase in extracellular glycine concentration by treatment with a glycine transporter 1 (GlyT1)-selective inhibitor, NFPS ethyl ester, significantly decreased the cerebellar localization of [11C]L-703,717 in rats. D-serine is known to be concentrated in mammalian forebrain regions. The lack of D-serine detection in the cerebellum may be due to the fact that it has the highest enzymatic activity of D-amino acid oxidase (DAO). It was found that the cerebellar localization of [11C]L-703,717 is greatly diminished in mutant mice lacking DAO, in which D-serine content in the cerebellum is drastically increased from a nondetectable level in normal mice. These studies indicate that [11C]L-703,717 is susceptible to inhibition by glycine site agonists in its in vivo binding, and suggest that regional differences in inhibitions by endogenous agonists may be a crucial factor in the site- and subunit-specific binding of this glycine-site antagonist. | |||||
| 書誌情報 |
Synapse 巻 50, p. 130-136, 発行日 2003-12 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0887-4476 | |||||
