Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening.

@article{Tournier2011TransportOS,
  title={Transport of selected PET radiotracers by human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2): an in vitro screening.},
  author={Nicolas Tournier and H{\'e}ric Valette and M. A. Peyronneau and Wadad Saba and S{\'e}bastien Goutal and Bertrand Kuhnast and Fr{\'e}d{\'e}ric Doll{\'e} and J. -M. Scherrmann and Salvatore Cisternino and Michel Bottlaender},
  journal={Journal of nuclear medicine : official publication, Society of Nuclear Medicine},
  year={2011},
  volume={52 3},
  pages={415-23}
}
UNLABELLED Radiolabeled compounds used for brain imaging with PET must readily cross the blood-brain barrier (BBB) to reach their target. Efflux transporters at the BBB-P-glycoprotein (P-gp) and the breast cancer resistance protein (BCRP)-could limit their uptake by the brain. METHODS We developed and validated an in vitro model using MDCKII cells transfected with human multidrug resistance (MDR1) or BCRP genes and assessed the transport of selected PET ligands by the concentration… CONTINUE READING
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