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ABC transporter dependent brain uptake of the 5-HT1B receptor radioligand [11C]AZ10419369
https://repo.qst.go.jp/records/47132
https://repo.qst.go.jp/records/47132c211aab0-0fc4-44a0-8ae9-174bddba34bd
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2015-05-11 | |||||
| タイトル | ||||||
| タイトル | ABC transporter dependent brain uptake of the 5-HT1B receptor radioligand [11C]AZ10419369 | |||||
| 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 |
Tóth, Miklós
× Tóth, Miklós× Häggkvist, Jenny× Varrone, Andrea× J, Finnema Sjoerd× Doorduin, Janine× Tokunaga, Masaki× Higuchi, Makoto× Gulyás, Balázs× Halldin, Christer× 徳永 正希× 樋口 真人 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Background We have explored the possibility that the serotonin 1B receptor radioligand [11C]AZ10419369 is a substrate for adenosine triphosphate (ATP)-binding cassette (ABC) transporters, such as P-glycoprotein (P-gp), Mrp4, and Bcrp, in rodents and whether there is a species difference regarding its blood-brain barrier (BBB) penetration. Methods In a series of preclinical positron emission tomography measurements, we have administered [11C]AZ10419369 to mice, rats, and guinea pigs under baseline conditions and, on separate experimental days, after administration of the ABC transporter inhibitor, cyclosporin A (CsA). Results During baseline conditions, the brain uptake was low in mice and rats, but not in guinea pigs. After CsA pretreatment, the peak whole brain uptake values of [11C]AZ10419369 increased by 207% in mice, 94% in rats, and 157% in guinea pigs. Binding potentials (BPND) could not be estimated during baseline conditions in mice and rats. After CsA pretreatment, the highest BPND values were obtained in the striatum and thalamus (BPND ≈ 0.4) in mice, while in rats, the highest binding areas were the striatum, thalamus, hypothalamus, and periaqueductal gray (BPND ≈ 0.5). In guinea pigs, we did not find any significant changes in BPND between baseline and CsA pretreatment, except in the striatum. Conclusions The results indicate that BBB penetration of [11C]AZ10419369 was hindered by ABC transporter activity in mouse, rat, and guinea pig. This study highlights the importance of ABC transporters in the design of preclinical positron emission tomography (PET) studies. |
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| 書誌情報 |
EJNMMI Research 巻 4, 号 1, p. 64, 発行日 2014-11 |
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| 出版者 | ||||||
| 出版者 | Springer | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 2191-219X | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1186/s13550-014-0064-0 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | http://link.springer.com/article/10.1186%2Fs13550-014-0064-0 | |||||
| 関連名称 | http://link.springer.com/article/10.1186%2Fs13550-014-0064-0 | |||||
