Banister, Samuel D
Beinat, Corinne
Wilkinson, Shane M
Shen, Bin
Bartoli, Cecilia
Selleri, Silvia
Da Pozzo, Eleonora
Martini, Claudia
Chin, Frederick T
Kassiou, Michael
2015-02-07
<p>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 = 0.13 nM). Additionally, all analogues increased pregnenolone biosynthesis (134–331% above baseline) in a rat C6 glioma cell steroidogenesis assay.</p>
https://doi.org/10.1016/j.ejmech.2015.02.004
oai:zenodo.org:16274
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Eur J Med Chem. , 93, 392-400, (2015-02-07)
translocator protein
pyrazolo[1,5-a]pyrimidine
DPA-714
steroid
positron emission tomography
Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).
info:eu-repo/semantics/article