WEKO3
アイテム
High occupancy of sigma-1 receptors in the human brain after single oral administration of donepezil: A positron emission tomography study usig [11C]SA4503
https://repo.qst.go.jp/records/45609
https://repo.qst.go.jp/records/4560903ab27db-7739-4057-8c2f-431f48d1a03c
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2009-08-18 | |||||
| タイトル | ||||||
| タイトル | High occupancy of sigma-1 receptors in the human brain after single oral administration of donepezil: A positron emission tomography study usig [11C]SA4503 | |||||
| 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 |
Ishikawa, Masatomo
× Ishikawa, Masatomo× Sakata, Muneyuki× Ishii, Kenji× Kimura, Yuichi× Oda, Keiichi× Toyohara, Jun× Wu, Jin× Ishiwata, Kiichi× Iyo, Masaomi× Hashimoto, Kenji× 坂田 宗之× 石井 賢二× 木村 裕一× 織田 圭一× 石渡 喜一× 橋本 謙二 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The acetylcholinesterase (AChE) inhibitor donepezil is also a sigma1 receptor agonist. We examined whether donepezil binds to sigma1 receptors in the living human brain after a single oral administration. Dynamic positron emission tomography (PET) data acquisition using the selective sigma1 receptor ligand [11C]SA4503 was performed to evaluate quantitatively the binding of [11C]SA4503 to sigma1 receptors in eight healthy male volunteers. Each subject had a PET scan before and after receiving a single dose of donepezil (5 or 10 mg). The binding potential of [11C]SA4503 was calculated. Doses of 5 mg and 10 mg donepezil bound to sigma1 receptors in the human brain with occupancies of ~60% and ~75%, respectively, in a dose-dependent manner. This study demonstrated that donepezil binds to sigma1 receptors in the living human brain at therapeutic doses. Therefore, sigma1 receptors may be implicated in the pharmacological mechanism of donepezil in the human brain. | |||||
| 書誌情報 |
The International Journal of Neuropsychopharmacology 巻 12, 号 8, p. 1127-1131, 発行日 2009-07 |
|||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1461-1457 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1017/s1461145709990204 | |||||
