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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 | Synthesis and evaluation of 3-(4-chlorobenzyl)-8-[11C]methoxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one: a PET tracer for imaging sigma(1) receptors. |
| 掲載誌名 | 正式名：Nuclear medicine and biology ISSNコード：09698051 |
| 出版社 | ELSEVIER SCIENCE INC |
| 巻・号・頁 | 29(4),469-76頁 |
| 著者・共著者 | Ming-Rong Zhang,Terushi Haradahira,Jun Maeda,Takashi Okauchi,Kouichi Kawabe,Takayo Kida,Shigeru Obayashi,Kazutoshi Suzuki,Tetsuya Suhara |
| 発行年月 | 2002/05 |
| 概要 | 3-(4-Chlorobenzyl)-8-methoxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one (1), a putative dopamine D(4) receptor antagonist (k(i) = 8.7 nM), was labeled by positron-emitter (11C) and its pharmacological evaluation was carried out with in vitro quantitative autoradiography and positron emission tomography (PET). 11C-Methylation of a corresponding desmethyl precursor (2) with [11C]CH(3)I gave [11C]1 with>or=98% of radiochemical purity after HPLC purification and 67-90 GBq/micromol of specific activity at the end of synthesis. The in vitro autoradiography using rat brain sections demonstrated that [11C]1 shows no specific binding to the D(4) receptors, but a high specific binding to sigma(1) receptors (IC(50) = 105 nM). In the PET study with monkey brain, [11C]1 was highly taken up by the brain andtrapped in the brain for at least 90 min. The distribution pattern of radioactivity in the brain was striatum>thalamus>frontal cortex>cerebellum, which was same as the result of in vitro autoradiography. Pre-treatment with non-radioactive 1 (1 mg/kg) produced a significant reduction of radioactivity in all the regions including the cerebellum. Pre-treatment with (+)pentazocine (1 m |
| DOI | 10.1016/S0969-8051(02)00293-7 |
| PMID | 12031882 |