@misc{oai:repo.qst.go.jp:00069508,
 author = {Saijo, Takeaki and Maeda, Jun and Okauchi, Takashi and Suzuki, Masayuki and Suzuki, Kazutoshi and Higuchi, Makoto and Suhara, Tetsuya and et.al and 西條 武明 and 前田 純 and 岡内 隆 and 鈴木 正幸 and 鈴木 和年 and 樋口 真人 and 須原 哲也},
 month = {Nov},
 note = {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., 第23回日本薬物動態学会},
 title = {APPLICATION OF SMALL ANIMAL POSITRON EMISSION TOMOGRAPHIC IMAGING TO PRECLINICAL ASSESSMENT OF DRUGS ACTING ON SEROTONIN TRANSPORTER},
 year = {2008}
}