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APPLICATION OF SMALL ANIMAL POSITRON EMISSION TOMOGRAPHIC IMAGING TO PRECLINICAL ASSESSMENT OF DRUGS ACTING ON SEROTONIN TRANSPORTER
https://repo.qst.go.jp/records/69508
https://repo.qst.go.jp/records/69508094eb9d1-0405-4e88-b73d-2323674d4867
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2008-10-08 | |||||
| タイトル | ||||||
| タイトル | APPLICATION OF SMALL ANIMAL POSITRON EMISSION TOMOGRAPHIC IMAGING TO PRECLINICAL ASSESSMENT OF DRUGS ACTING ON SEROTONIN TRANSPORTER | |||||
| 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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 |
Saijo, Takeaki
× Saijo, Takeaki× Maeda, Jun× Okauchi, Takashi× Suzuki, Masayuki× Suzuki, Kazutoshi× Higuchi, Makoto× Suhara, Tetsuya× et.al× 西條 武明× 前田 純× 岡内 隆× 鈴木 正幸× 鈴木 和年× 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 | We investigated the comparability of pharmacodynamic parameters for the occupancy of serotonin transporter (5-HTT) by therapeutic agents in rat positron emission tomographic (PET) studies with our predetermined data from ex vivo animal experiments and clinical PET scans, in order to examine the utility of high-resolution PET imaging system for preclinical characterization of 5-HTT inhibitors. Rats were treated with varying doses of high-affinity inhibitors of 5-HTT, including fluvoxamine and a newly developed compound, Wf-516, and subsequently underwent PET scans with [11C] 3-amino-4-(2-dimethylaminomethyl-phenylsulfanyl)-benzonitrile ([11C]DASB). PET images indicated a reduction of [11C]DASB binding to 5-HTT as a function of the administered doses and/or plasma concentrations of fluvoxamine and Wf-516, and the ED50 estimates of these drugs were in general agreement with those estimated by our previous ex vivo measurements in rats. Moreover, the EC50 value of fluvoxamine in plasma determined here (6.1 ng/mL) was nearly equivalent to the value determined in human PET studies (4.6 ng/mL). These findings support the view that the use of small animal PET facilitates a quantitative comparison of in-development drugs targeting 5-HTT with known inhibitors and a predictive estimation of their doses exerting therapeutic effects in humans. | |||||
| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | 第23回日本薬物動態学会 | |||||
| 発表年月日 | ||||||
| 日付 | 2008-11-01 | |||||
| 日付タイプ | Issued | |||||
