10.1016/j.ejmech.2015.02.004
https://zenodo.org/records/16274
oai:zenodo.org:16274
Banister, Samuel D
Samuel D
Banister
Department of Radiology, Stanford University School of Medicine, Stanford, CA 94305, USA and School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia
Beinat, Corinne
Corinne
Beinat
Department of Radiology, Stanford University School of Medicine, Stanford, CA 94305, USA and School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia
Wilkinson, Shane M
Shane M
Wilkinson
School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia
Shen, Bin
Bin
Shen
Department of Radiology, Stanford University School of Medicine, Stanford, CA 94305, USA
Bartoli, Cecilia
Cecilia
Bartoli
Department of Pharmaceutical Sciences, University of Florence, Via U. Schiff, 650019 Polo Scientifico Sesto Fiorentino, Italy
Selleri, Silvia
Silvia
Selleri
Department of Pharmaceutical Sciences, University of Florence, Via U. Schiff, 650019 Polo Scientifico Sesto Fiorentino, Italy
Da Pozzo, Eleonora
Eleonora
Da Pozzo
Department of Pharmacy, University of Pisa, Via Bonanno 6, 56127 Pisa, Italy
Martini, Claudia
Claudia
Martini
Department of Pharmacy, University of Pisa, Via Bonanno 6, 56127 Pisa, Italy
Chin, Frederick T
Frederick T
Chin
Department of Radiology, Stanford University School of Medicine, Stanford, CA 94305, USA
Kassiou, Michael
Michael
Kassiou
School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia and Faculty of Health Sciences, The University of Sydney, Sydney, NSW 2006, Australia
Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).
Zenodo
2015
translocator protein
pyrazolo[1,5-a]pyrimidine
DPA-714
steroid
positron emission tomography
2015-02-07
https://zenodo.org/communities/inmind
https://zenodo.org/communities/eu
Creative Commons Attribution 4.0 International
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.
European Commission
10.13039/501100000780
278850
Imaging of Neuroinflammation in Neurodegenerative Diseases