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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 | 11C-AC-5216: a novel PET ligand for peripheral benzodiazepine receptors in the primate brain. |
| 掲載誌名 | 正式名：Journal of nuclear medicine : official publication, Society of Nuclear Medicine ISSNコード：01615505 |
| 出版社 | SOC NUCLEAR MEDICINE INC |
| 巻・号・頁 | 48(11),1853-61頁 |
| 著者・共著者 | Ming-Rong Zhang,Katsushi Kumata,Jun Maeda,Kazuhiko Yanamoto,Akiko Hatori,Maki Okada,Makoto Higuchi,Shigeru Obayashi,Tetsuya Suhara,Kazutoshi Suzuki |
| 発行年月 | 2007/11 |
| 概要 | UNLABELLED: Developing a PET ligand for imaging of the peripheral benzodiazepine receptor (PBR; Translocator Protein [18 kDa]TSPO) is of great importance for studying its role in glial cells in the injured brain and in neurodegenerative disorders, such as Alzheimer's disease. The aim of this study was to synthesize and evaluate N-benzyl-N-ethyl-2-(7-(11)C-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide ((11)C-AC-5216) as a PET ligand for imaging PBR in the primate brain. METHODS: AC-5216 and its desmethyl precursor (compound 1) were synthesized starting from commercially available compounds. The radiosynthesis of (11)C-AC-5216 was performed through the reaction of compound 1 with (11)C-CH(3)I in the presence of NaH. The in vivo brain regional distribution was determined in mice (dissection) and a monkey (PET). RESULTS: (11)C-AC-5216 (800-1,230 MBq; n = 25) was obtained with a radiochemical purity of 98% and a specific activity of 85-130 GBq/mumol at the end of synthesis. After injection of (11)C-AC-5216 into mice, a high accumulation of radioactivity was found in the lungs, heart, adrenal glands, and other PBR-rich organs. In the mouse brain, high radioactivity was obser |
| DOI | 10.2967/jnumed.107.043505 |
| PMID | 17978354 |