WEKO3
アイテム
Synthesis and evaluation of 1-(cyclopropylmethyl)-4-(4-[11C]methoxyphenyl)- piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile ([11C]CMDC) for PET imaging of metabotropic glutamate receptor 2 in the rat brain
https://repo.qst.go.jp/records/47643
https://repo.qst.go.jp/records/4764374cf1af8-0ad9-4815-a60b-f2157c909071
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-02-15 | |||||
| タイトル | ||||||
| タイトル | Synthesis and evaluation of 1-(cyclopropylmethyl)-4-(4-[11C]methoxyphenyl)- piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile ([11C]CMDC) for PET imaging of metabotropic glutamate receptor 2 in the rat brain | |||||
| 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 |
Ma, Yufei
× Ma, Yufei× Kumata, Katsushi× Yui, Joji× Zhang, Yiding× Yamasaki, Tomoteru× Hatori, Akiko× Fujinaga, Masayuki× Nengaki, Nobuki× Xie, Lin× Wang, Hui× Zhang, Ming-Rong× 熊田 勝志× 張 一鼎× 山崎 友照× 羽鳥 晶子× 藤永 雅之× 念垣 信樹× 謝 琳× 張 明栄 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Brain metabotropic glutamate receptor 2 (mGluR2) has been proposed as a therapeutic target for the treatment of schizophrenia-like symptoms arising from increased glutamate transmission in the forebrain. However, there does not exist a reliable tool for the study of mGluR2 in human neuroimaging. The purpose of this study was to radiosynthesize 1-(cyclopropylmethyl)-4-(4-[11C]methoxyphenyl)piperidin-1-yl-2-oxo-1,2-dihydropyridine- 3-carbonitrile ([11C]CMDC) and evaluate its potential as a positron emission tomography (PET) radiotracer for imaging mGluR2 in the rat brain. CMDC, a positive allosteric modulator of mGluR2, showed potent functional activity (EC50: 98 nM) for human mGluR2 in vitro. [11C]CMDC was synthesized by O-[11C]methylation of 1-(cyclopropylmethyl)-4- (4-hydroxyphenyl)piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile (1) with [11C]methyl iodide. [11C]CMDC (2.2 ± 0.9 GBq; n = 20) was obtained from [11C]CO2 of 14.0–17.8 GBq with >98% radiochemical purity and 86–150 GBq/μmol specific activity at the end of synthesis. In vitro autoradiography indicated that [11C]CMDC binding was expressed (>50% of total binding) in mGluR2-rich brain regions including the cerebral cortex, striatum and hippocampus. However, small-animal PET showed low in vivo specific binding of [11C]CMDC in the rat brain. While [11C]CMDC has limited potential as a PET tracer for brain mGluR2, it can be used to develop new radiotracers with improved behaviors. | |||||
| 書誌情報 |
Bioorganic & Medicinal Chemistry 巻 25, 号 3, p. 1014-1021, 発行日 2016-12 |
|||||
| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.bmc.2016.12.011 | |||||
