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Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [11C]GF120918 by PET in mice
https://repo.qst.go.jp/records/45987
https://repo.qst.go.jp/records/4598725a0af2d-53b3-467d-8190-0560ee10d81c
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2011-01-25 | |||||
| タイトル | ||||||
| タイトル | Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [11C]GF120918 by PET in mice | |||||
| 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 |
Kawamura, Kazunori
× Kawamura, Kazunori× Yamasaki, Tomoteru× Konno, Fujiko× Yui, Joji× Hatori, Akiko× Yanamoto, Kazuhiko× Wakizaka, Hidekatsu× Takei, Makoto× Kimura, Yuichi× Fukumura, Toshimitsu× Zhang, Ming-Rong× 河村 和紀× 山崎 友照× 昆野 富士子× 由井 譲二× 羽鳥 晶子× 柳本 和彦× 脇坂 秀克× 武井 誠× 木村 裕一× 福村 利光× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Purpose GF120918 has a high inhibitory effect on P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). We developed [11C]GF120918 as a positron emission tomography (PET) probe to assess if dual modulation of P-gp and BCRP is useful to evaluate brain penetration. Procedures PET studies using [11C]GF120918 were conducted on P-gp and/or Bcrp knockout mice as well as wild-type mice. Results In PET studies, the AUCbrain [0–60 min] and K 1 value in P-gp/Bcrp knockout mice were nine- and 26-fold higher than that in wild-type mice, respectively. These results suggest that brain penetration of [11C]GF120918 is related to modulation of P-gp and BCRP and is limited by two transporters working together. Conclusions PET using [11C]GF120918 may be useful for evaluating the function of P-gp and BCRP. PET using P-gp/Bcrp knockout mice may be an effective method to understand the overall contributions the functions of P-gp and BCRP. |
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| 書誌情報 |
Molecular Imaging and Biology 巻 13, 号 1, p. 152-160, 発行日 2010-04 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1536-1632 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1007/s11307-010-0313-1 | |||||
