1262278-66-9Relevant articles and documents
Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO)
Banister, Samuel D.,Beinat, Corinne,Wilkinson, Shane M.,Shen, Bin,Bartoli, Cecilia,Selleri, Silvia,Da Pozzo, Eleonora,Martini, Claudia,Chin, Frederick T.,Kassiou, Michael
, p. 392 - 400 (2015)
Sixteen new phenyl alkyl ether derivatives (12, 14-28) of the 5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-ylacetamide (DPA) class were synthesized and evaluated in a competition binding assay against [3H]PK11195 using 18 kDa translocator protein (TSPO) derived from rat kidney mitochondrial fractions. All analogues showed superior binding affinities for TSPO compared to DPA-713 (5) and DPA-714 (6). Picomolar affinities were observed for this class of TSPO ligands in this assay for the first time, with phenethyl ether 28 showing the greatest affinity (Ki Combining double low line 0.13 nM). Additionally, all analogues increased pregnenolone biosynthesis (134-331% above baseline) in a rat C6 glioma cell steroidogenesis assay.