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  • Title: Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).
    Author: Banister SD, Beinat C, Wilkinson SM, Shen B, Bartoli C, Selleri S, Da Pozzo E, Martini C, Chin FT, Kassiou M.
    Journal: Eur J Med Chem; 2015 Mar 26; 93():392-400. PubMed ID: 25725375.
    Abstract:
    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 [(3)H]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 = 0.13 nM). Additionally, all analogues increased pregnenolone biosynthesis (134-331% above baseline) in a rat C6 glioma cell steroidogenesis assay.
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