Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).

Banister, Sd; Beinat, C; Wilkinson, Sm; Shen, B; Bartoli, C; Selleri, S; Da Pozzo, E; Martini, C; Chin, Ft; Kassiou, M

doi:10.1016/j.ejmech.2015.02.004

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.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/744875

Autori interni:	DA POZZO, ELEONORA MARTINI, CLAUDIA
Autori:	Banister SD;Beinat C;Wilkinson SM;Shen B;Bartoli C;Selleri S;Da Pozzo E;Martini C;Chin FT;Kassiou M
Titolo:	Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).
Anno del prodotto:	2015
Digital Object Identifier (DOI):	10.1016/j.ejmech.2015.02.004
Appare nelle tipologie:	1.1 Articolo in rivista

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