@article{oai:repo.qst.go.jp:00045951,
 author = {Yamasaki, Tomoteru and Kawamura, Kazunori and Hatori, Akiko and Yui, Joji and Yanamoto, Kazuhiko and Yoshida, Yuichiro and Ogawa, Masanao and Nengaki, Nobuki and Wakizaka, Hidekatsu and Fukumura, Toshimitsu and Zhang, Ming-Rong and 山崎 友照 and 河村 和紀 and 羽鳥 晶子 and 由井 譲二 and 柳本 和彦 and 吉田 勇一郎 and 小川 政直 and 念垣 信樹 and 脇坂 秀克 and 福村 利光 and 張 明栄},
 issue = {11},
 journal = {Nuclear Medicine Communications},
 month = {Nov},
 note = {Objective: To evaluate the functions of P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) in human colon adenocarcinoma (Caco-2), we carried out an in-vitro study and a small animal positron emission tomography (PET) study using [11C]GF120918 (elacridar).
\nMethods: [11C]GF120918 was synthesized by reacting the desmethyl precursor with [11C]CH3I. An in-vitro study using [11C]GF120918 was carried out in Caco-2 and Madin–Darby canine kidney cells in the presence or absence of a transporter inhibitor (cyclosporine A and unlabeled GF120918). The biodistribution of radioactivity after the injection of [11C]GF120918 was determined in Caco-2-bearing mice using a small animal PET scanner.
\nResults: In Caco-2 cells expressing Pgp and BCRP, coincubation with unlabeled GF120918 caused an approximately two-fold increase in [11C]GF120918 uptake compared with that of the control ([11C]GF120918 only). In Caco-2-bearing mice, PET results indicated that [11C]GF120918 uptake in the tumor was low, but was significantly increased by treatment with unlabeled GF120918. In metabolite analysis, the radioactive component in the tumor almost corresponded to intact [11C]GF120918.
\nConclusion: A PET study combining the administration of [11C]GF120918 with unlabeled GF120918 may be a useful tool for evaluating the functions of Pgp and BCRP in tumors.},
 pages = {985--993},
 title = {PET study on mice bearing human colon adenocarcinoma cells using [11C]GF120918, a dual radioligand for P-glycoprotein and breast cancer resistance protein},
 volume = {31},
 year = {2010}
}