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Synthesis and evaluation of 1-[2-(4-[11C] methoxyphenyl)phenyl]piperazine for imaging of the serotonin 5-HT7 receptor in the rat brain
https://repo.qst.go.jp/records/47342
https://repo.qst.go.jp/records/47342ea9777a8-b2cc-4efd-8190-5f745cae2d33
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2015-12-10 | |||||
| タイトル | ||||||
| タイトル | Synthesis and evaluation of 1-[2-(4-[11C] methoxyphenyl)phenyl]piperazine for imaging of the serotonin 5-HT7 receptor 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 |
Shimoda, Yoko
× Shimoda, Yoko× Yui, Joji× Xie, Lin× Fujinaga, Masayuki× Yamasaki, Tomoteru× Ogawa, Masanao× Nengaki, Nobuki× Kumata, Katsushi× Hatori, Akiko× Kawamura, Kazunori× Zhang, Ming-Rong× 下田 陽子× 由井 譲二× 謝 琳× 藤永 雅之× 山崎 友照× 小川 政直× 念垣 信樹× 熊田 勝志× 羽鳥 晶子× 河村 和紀× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 1-[2-(4-Methoxyphenyl)phenyl]piperazine (4) is a potent serotonin 5-HT7 receptor antagonist (Ki = 2.6 nM) with a low binding affinity for the 5-HT1A receptor (Ki = 476 nM). As a potential positron emission tomography (PET) radiotracer for the 5-HT7 receptor, [11C]4 was synthesized at high radiochemical yield and specific activity, by O-[11C]methylation of 20-(piperazin-1-yl)-[1,10-biphenyl]-4-ol (6) with [11C]methyl iodide. Autoradiography revealed that [11C]4 showed in vitro specific binding with 5-HT7 in the rat brain regions, such as the thalamus which is a region with high 5-HT7 expression. Metabolite analysis indicated that intact [11C]4 in the brain exceeded 90% of the radioactive components at 15 min after the radiotracer injection, although two radiolabeled metabolites were found in the rat plasma. The PET study of rats showed moderated uptake of [11C]4 in the brain (1.2 SUV), but no significant regional difference in radioactivity in the brain. Pretreatment with 5-HT7-selective antagonist SB269970 (3) did not decrease the uptake of [11C]4 in the rat brain. Further studies are warranted that focus on the development of PET ligand candidates with higher binding affinity for 5-HT7 and higher in vivo stability in brain than 4. |
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| 書誌情報 |
Bioorganic & Medicinal Chemistry 巻 21, 号 17, p. 5316-5322, 発行日 2013-12 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0968-0896 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 23830697 | |||||
