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• W2324487612 abstract "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). Methods [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. Results 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. Conclusion 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." @default.
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• W2324487612 date "2010-11-01" @default.
• W2324487612 modified "2023-09-24" @default.
• W2324487612 title "PET study on mice bearing human colon adenocarcinoma cells using [11C]GF120918, a dual radioligand for P-glycoprotein and breast cancer resistance protein" @default.
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• W2324487612 doi "https://doi.org/10.1097/mnm.0b013e32833fbf87" @default.
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