Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier.

@article{Drner2009SynthesisAS,
  title={Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier.},
  author={Bernd D{\"o}rner and Claudia Kuntner and Jens P. Bankstahl and Marion Bankstahl and Johann Stanek and Thomas Wanek and Gloria Stundner and Severin Mairinger and Wolfgang L{\"o}scher and Markus M{\"u}ller and Oliver Langer and Thomas Erker},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 19},
  pages={6073-82}
}
With the aim to develop a positron emission tomography (PET) tracer to assess the distribution of P-glycoprotein (P-gp) at the blood-brain barrier (BBB) in vivo, the potent third-generation P-gp inhibitor elacridar (1) was labeled with (11)C by reaction of O-desmethyl 1 with [(11)C]-methyl triflate. In vitro autoradiography and small-animal PET imaging of [(11)C]-1 was performed in rats (n = 3), before and after administration of unlabeled 1, as well as in wild-type, Mdr1a/b((-/-)) and Bcrp1… CONTINUE READING

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