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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. \nProcedures \nPET studies using [11C]GF120918 were conducted on P-gp and/or Bcrp knockout mice as well as wild-type mice. \nResults \nIn PET studies, the AUCbrain [0\u0026#8211;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. \nConclusions \nPET using [11C]GF120918 may be useful for evaluating the function of P-gp and BCRP. 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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) | |||||
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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 |