Development of N-Methyl-(2-arylquinolin-4-yl)oxypropanamides as Leads to PET Radioligands for Translocator Protein (18 kDa)

@inproceedings{Brouwer2014DevelopmentON,
  title={Development of N-Methyl-(2-arylquinolin-4-yl)oxypropanamides
as Leads to PET Radioligands for Translocator Protein (18 kDa)},
  author={Chad Brouwer and Kimberly J. Jenko and Sami S. Zoghbi and Robert B. Innis and Victor W. Pike},
  booktitle={Journal of medicinal chemistry},
  year={2014}
}
Translocator protein (18 kDa), known as TSPO, is a recognized biomarker of neuroinflammation. Radioligands with PET accurately quantify TSPO in neuroinflammatory conditions. However, the existence of three human TSPO genotypes that show differential affinity to almost all useful TSPO PET radioligands hampers such studies. There is an unmet need for genotype-insensitive, high-affinity, and moderately lipophilic TSPO ligands that may serve as leads for PET radioligand development. To address this… CONTINUE READING