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オオバヤシ シゲル
OBAYASHI Shigeru
大林 茂 所属 埼玉医科大学 医学部 総合医療センター リハビリテーション科 職種 教授 |
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| 論文種別 | 学術雑誌(原著) |
| 言語種別 | |
| 査読の有無 | 査読あり |
| 表題 | Synthesis and preliminary PET study of the 5-HT<inf>7</inf>receptor antagonist [11C]DR4446 |
| 掲載誌名 | 正式名：Journal of Labelled Compounds and Radiopharmaceuticals ISSNコード：03624803 |
| 巻・号・頁 | 45(10),857-866頁 |
| 著者・共著者 | Ming Rong Zhang,Terushi Haradahira,Jun Maeda,Takashi Okauchi,Takayo Kida,Shigeru Obayashi,Kazutoshi Suzuki,Tetsuya Suhara |
| 発行年月 | 2002/09 |
| 概要 | DR4446 (1-methyl-2a-[4-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-5-yl)butyl]-2a, 3,4,5-tetrahydro-1H-benz[cd]indole-2-one) is a potent 5-HT7 receptor antagonist (Ki=9.7nM) with a high selectivity over other 5-HT family receptors (Ki for 5-HT1A: 770nM; for other 5-HT receptors:>1000 nM). As a positron emission tomography (PET) tracer for the 5-HT7 receptor, [11C]DR4446 was synthesized at high radiochemical purity (>98%) with specific activity of 73-120 GBq/μmol at the end of synthesis by the alkylation of the desmethyl precursor (1) with [11C]CH3I in the presence of NaH. A PET study in monkey demonstrated that [11C]DR4446 had good permeability into the brain, and had a specific binding component in the brain regions including the thalamus, possibly an area in the 5-HT7 receptors. Metabolite analysis showed that [11C]DR4446 was relatively stable and low percentages of two radio-labeled metabolites were detected in the plasma of monkey using HPLC. Copyright © 2002 John Wiley&Sons, Ltd. |
| DOI | 10.1002/jlcr.606 |