Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain.

@article{Tu2011RadiosynthesisAI,
  title={Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain.},
  author={Zhude Tu and Jinda Fan and Shihong Li and Lynne A. Jones and Jinquan Cui and Prashanth K. Padakanti and Jinbin Xu and Dexing Zeng and Kooresh I. Shoghi and Joel S. Perlmutter and Robert H. Mach},
  journal={Bioorganic & medicinal chemistry},
  year={2011},
  volume={19 5},
  pages={1666-73}
}
2-((4-(1-[(11)C]Methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)-quinoline (MP-10), a specific PDE10A inhibitor (IC(50)=0.18 nM with 100-fold selectivity over other PDEs), was radiosynthesized by alkylation of the desmethyl precursor with [(11)C]CH(3)I, ∼45% yield, >92% radiochemical purity, >370 GBq/μmol specific activity at end of bombardment (EOB). Evaluation in Sprague-Dawley rats revealed that [(11)C]MP-10 had highest brain accumulation in the PDE10A enriched-striatum, the 30 min… CONTINUE READING

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