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Occupancy of norepinephrine transporter by duloxetine in human brains measured by positron emission tomography with (S,S)-[18F]FMeNER-D2
https://repo.qst.go.jp/records/48726
https://repo.qst.go.jp/records/4872663892e10-8c24-4e12-a493-6ac1a0ba08de
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-04-15 | |||||
| タイトル | ||||||
| タイトル | Occupancy of norepinephrine transporter by duloxetine in human brains measured by positron emission tomography with (S,S)-[18F]FMeNER-D2 | |||||
| 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 |
Moriguchi, Sho
× Moriguchi, Sho× Takano, Harumasa× Kimura, Yasuyuki× Nagashima, Tomohisa× Takahata, Keisuke× Kubota, Manabu× Kitamura, Soichiro× Ishii, Tatsuya× Ichise, Masanori× Zhang, Ming-Rong× Shimada, Hitoshi× Mimura, Masaru× H., Meyer Jeffrey× Higuchi, Makoto× Suhara, Tetsuya× 森口 翔× 高野 晴成× 木村 泰之× 永嶌 朋久× 高畑 圭輔× 久保田 学× 北村 聡一郎× 石井 辰弥× 市瀬 正則× 張 明栄× 島田 斉× 三村 將× 樋口 真人× 須原 哲也 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Background: The norepinephrine transporter (NET) in the brain has been targeted in the treatment of psychiatric disorders. Duloxetine is a serotonin and norepinephrine reuptake inhibitor that has been widely used for the treatment of depression. However, the relationship between dose and plasma concentration of duloxetine and NET occupancy in the human brain has not been determined. In this study, we examined NET occupancy by different doses of duloxetine. Methods: We calculated NET occupancies from two positron emission tomography (PET) scans using (S,S)-[18F]FMeNER-D2 before and after a single oral dose of duloxetine (20 mg, n = 3; 40 mg, n = 3; 60 mg, n = 2). PET scans were performed from 120 to 180 min after an intravenous bolus injection of (S,S)-[18F]FMeNER-D2. Venous blood samples were taken to measure the plasma concentration of duloxetine just before and after the second PET scan. Results: NET occupancy by duloxetine was 29.7% at 20 mg, 30.5% at 40 mg, and 40.0% at 60 mg. The estimated dose of duloxetine inducing 50% NET occupancy (ED50) was 76.8 mg, and the estimated plasma drug concentration inducing 50% NET occupancy (EC50) was 58.0 ng/mL. Conclusions: NET occupancy by clinical doses of duloxetine was approximately 30–40% in human brain as estimated using PET with (S,S)-[18F]FMeNER-D2. |
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| 書誌情報 |
The International Journal of Neuropsychopharmacology 巻 20, 号 12, p. 957-962, 発行日 2017-07 |
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| 出版者 | ||||||
| 出版者 | Oxford University Press | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1461-1457 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 29016875 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1093/ijnp/pyx069 | |||||
