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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 sigma1 receptors
https://repo.qst.go.jp/records/44320
https://repo.qst.go.jp/records/44320307ab722-be8b-466b-939f-73321daf8d46
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-23 | |||||
| タイトル | ||||||
| タイトル | 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 sigma1 receptors | |||||
| 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 |
Zhang, Ming-Rong
× Zhang, Ming-Rong× Haradahira, Terushi× Maeda, Jun× Okauchi, Takashi× Kawabe, Koichi× Kida, Takayo× Obayashi, Shigeru× Suzuki, Kazutoshi× Suhara, Tetsuya× 張 明栄× 原田平 輝志× 前田 純× 岡内 隆× 大林 茂× 鈴木 和年× 須原 哲也 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 3-(4-Chlorobenzyl)-8-methoxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one (1), a putative dopamine D4 receptor antagonist (ki = 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]CH3I gave [11C]1 with >98% of radiochemical purity after HPLC purification and 67_90 GBq/mumol 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 D4 receptors, but a high specific binding to sigma1 receptors(IC50=105nM). In the PET study with monkey brain, [11C]1 was highly taken up by the brain and trapped 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 mg/kg),a selective sigma1 receptor agonist, also reduced the radioactivity in the same regions to a similar extent. These results indicate that [11C]1 may have some specific binding to the sigma1 receptors, which is consistent with the result of in vitro autoradiography. | |||||
| 書誌情報 |
Nuclear Medicine and Biology 巻 29, p. 469-476, 発行日 2002 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0969-8051 | |||||
