11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux.

@article{Zoghbi200811CloperamideAI,
  title={11C-loperamide and its N-desmethyl radiometabolite are avid substrates for brain permeability-glycoprotein efflux.},
  author={Sami S. Zoghbi and Jeih-San Liow and Fumihiko Yasuno and Jinsoo Hong and Edward W. Tuan and Neva Lazarova and Robert L. Gladding and Victor W. Pike and Robert B. Innis},
  journal={Journal of nuclear medicine : official publication, Society of Nuclear Medicine},
  year={2008},
  volume={49 4},
  pages={649-56}
}
UNLABELLED Loperamide, an opiate receptor agonist, does not cross the blood-brain barrier because it is a substrate for the permeability-glycoprotein (P-gp) efflux pump. We evaluated 11C-loperamide as a PET radiotracer to measure P-gp function in vivo. METHODS Monkeys were injected with 11C-loperamide, and PET brain images were acquired for 120 min. The baseline scans were followed by scans acquired after administration of either of 2 P-gp inhibitors, (2R)-anti-5-{3-[4-(10,11… CONTINUE READING

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