WEKO3
アイテム
Effect of Risperidone on High-Affinity State of Dopamine D2 Receptors:a PET Study with Agonist Ligand [11C](R)-2-CH3O-N-n-propylnorapomorphine
https://repo.qst.go.jp/records/46043
https://repo.qst.go.jp/records/46043fd577f96-9ed1-4f28-a97a-824f768c6cfb
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2011-05-23 | |||||
| タイトル | ||||||
| タイトル | Effect of Risperidone on High-Affinity State of Dopamine D2 Receptors:a PET Study with Agonist Ligand [11C](R)-2-CH3O-N-n-propylnorapomorphine | |||||
| 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 |
Kodaka, Fumitoshi
× Kodaka, Fumitoshi× Ito, Hiroshi× Takano, Harumasa× Takahashi, Hidehiko× Arakawa, Ryosuke× Miyoshi, Michie× Okumura, Masaki× Otsuka, Tatsui× Nakayama, Kazuhiko× Halldin, Christer× Farde, Lars× Suhara, Tetsuya× 小高 文聰× 伊藤 浩× 高野 晴成× 高橋 英彦× 荒川 亮介× 三好 美智恵× 奥村 正紀× 大塚 達以× ハルディン クリスタ× 須原 哲也 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The increased proportion of the high-affinity state of dopamine D2/3 receptors (D2,high) is assumed to correlate with dopamine hypersensitivity, implying a relationship with psychotic symptoms observed in psychiatric disorders such as schizophrenia. [11C](R)-2-CH3O-N-n-propylnorapomorphine ([11C]MNPA), which has an agonistic property to dopamine D2 receptors (D2Rs), is expected to bind preferentially to D2,high. The occupancy of dopamine D2Rs by antagonists to receptors has not been investigated using [11C]MNPA. We compared dopamine D2R occupancies by risperidone, an antagonist to receptors, between [11C]MNPA and [11C]raclopride to confirm whether risperidone occupies D2,high and D2,low at almost identical proportions. PET studies were performed on 11 healthy men under resting condition and following oral administration of a single dose of risperidone (0.5-2.0 mg). Striatal receptor occupancy for each radioligand was calculated. The relationship between dose or plasma concentration of risperidone and dopamine D2R occupancy was calculated. Striatal dopamine D2R occupancies measured with [11C]MNPA and [11C]raclopride were 22-65% and 24-69%, respectively. In the striatum, ED50 values measured with [11C]MNPA and [11C]raclopride were 0.98 and 1.03 mg, respectively. The striatal ED50 values as calculated from plasma concentration were 9.15 ng/ml and 8.01 ng/ml, respectively. Almost identical occupancies and ED50 values were observed between the two radioligands, indicating that risperidone bound to D2,high and D2,low at almost identical proportions in a dose-dependent manner. | |||||
| 書誌情報 |
The International Journal of Neuropsychopharmacology 巻 14, 号 1, p. 83-89, 発行日 2011-02 |
|||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1461-1457 | |||||
