@article{oai:repo.qst.go.jp:00045987,
 author = {Kawamura, Kazunori and Yamasaki, Tomoteru and Konno, Fujiko and Yui, Joji and Hatori, Akiko and Yanamoto, Kazuhiko and Wakizaka, Hidekatsu and Takei, Makoto and Kimura, Yuichi and Fukumura, Toshimitsu and Zhang, Ming-Rong and 河村 和紀 and 山崎 友照 and 昆野 富士子 and 由井 譲二 and 羽鳥 晶子 and 柳本 和彦 and 脇坂 秀克 and 武井 誠 and 木村 裕一 and 福村 利光 and 張 明栄},
 issue = {1},
 journal = {Molecular Imaging and Biology},
 month = {Apr},
 note = {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.},
 pages = {152--160},
 title = {Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [11C]GF120918 by PET in mice},
 volume = {13},
 year = {2010}
}