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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 | 英語 |
| 査読の有無 | 査読あり |
| 表題 | Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain. |
| 掲載誌名 | 正式名：Journal of medicinal chemistry ISSNコード：00222623 |
| 出版社 | AMER CHEMICAL SOC |
| 巻・号・頁 | 47(9),2228-35頁 |
| 著者・共著者 | Ming-Rong Zhang,Jun Maeda,Masanao Ogawa,Junko Noguchi,Takehito Ito,Yuichiro Yoshida,Takashi Okauchi,Shigeru Obayashi,Tetsuya Suhara,Kazutoshi Suzuki |
| 発行年月 | 2004/04 |
| 概要 | To develop a positron emission tomography (PET) ligand for imaging the 'peripheral benzodiazepine receptor' (PBR) in brain and elucidating the relationship between PBR and brain diseases, four analogues (4-7) of N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide (2) were synthesized and evaluated as ligands for PBR. Of these compounds, fluoromethyl (4) and fluoroethyl (5) analogues had similar or higher affinities for PBR than the parent compound 2 (K(i) = 0.16 nM for PBR in rat brain sections). Iodomethyl analogue 6 displayed a moderate affinity, whereas tosyloxyethyl analogue 7 had weak affinity. Radiolabeling was performed for the fluoroalkyl analogues 4 and 5 using fluorine-18 ((18)F, beta(+); 96.7%, T(1/2) = 109.8 min). Ligands [(18)F]4 and [(18)F]5 were respectively synthesized by the alkylation of desmethyl precursor 3 with [(18)F]fluoromethyl iodide ([(18)F]8) and 2-[(18)F]fluoroethyl bromide ([(18)F]9). The distribution patterns of [(18)F]4 and [(18)F]5 in mice were consistent with the known distribution of PBR. However, compared with [(18)F]5, [(18)F]4 displayed a high uptake in the bone of mice. The PET image of [(18)F]4 for monkey brain also showed significan |
| DOI | 10.1021/jm0304919 |
| PMID | 15084121 |