Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand.

@article{James2005SynthesisAI,
  title={Synthesis and in vivo evaluation of a novel peripheral benzodiazepine receptor PET radioligand.},
  author={Michelle L. James and Roger R. Fulton and David J Henderson and Stefan Eberl and Steven R. Meikle and Sally A Thomson and Robin D. Allan and Fr{\'e}d{\'e}ric Doll{\'e} and Michael J. Fulham and Michael Kassiou},
  journal={Bioorganic & medicinal chemistry},
  year={2005},
  volume={13 22},
  pages={6188-94}
}
The novel pyrazolopyrimidine ligand, N,N-diethyl-2-[2-(4-methoxyphenyl)-5,7-dimethyl-pyrazolo[1,5-a]pyrimidin-3-yl]-acetamide 1 (DPA-713), has been reported as a potent ligand for the peripheral benzodiazepine receptor (PBR) displaying an affinity of K(i)=4.7 nM. In this study, 1 was successfully synthesised and demethylated to form the phenolic derivative 6 as precursor for labelling with carbon-11 (t(1/2) = 20.4 min). [11C]1 was prepared by O-alkylation of 6 with [11C]methyl iodide. The… CONTINUE READING
29 Citations
0 References
Similar Papers

Citations

Publications citing this paper.
Showing 1-10 of 29 extracted citations

Similar Papers

Loading similar papers…