868072-17-7Relevant articles and documents
Efficient tritiation of the translocator protein (18kDa) selective ligand DPA-714
Damont, Annelaure,Garcia-Argote, Sébastien,Buisson, David-Alexandre,Rousseau, Bernard,Dollé, Frédéric
, p. 1 - 6 (2015)
DPA-714 (N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide) is a recently discovered fluorinated ligand of the translocator protein 18 kDa (TSPO). Labelled with the short-lived positron emitter fluorine-18, th
Targeting Mitochondria in Tumor-Associated Macrophages using a Dendrimer-Conjugated TSPO Ligand that Stimulates Antitumor Signaling in Glioblastoma
Kannan, Rangaramanujam M.,Kannan, Sujatha,Liaw, Kevin,Sharma, Anjali,Sharma, Rishi,Slusher, Barbara S.,Thomas, Ajit G.
, p. 3909 - 3922 (2020/10/18)
Mitochondria mediate critical cellular processes, including proliferation, apoptosis, and immune responses; as such, their dysfunction is pathogenic in many neurodegenerative disorders and cancers. In glioblastoma, targeted delivery of mitochondria-focuse
Synthesis and evaluation of novel potent TSPO PET ligands with 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamide
Hieu Tran, Van,Park, Hyunjun,Park, Jaekyung,Kwon, Young-Do,Kang, Shinwoo,Ho Jung, Jae,Chang, Keun-A,Chul Lee, Byung,Lee, Sang-Yoon,Kang, Soosung,Kim, Hee-Kwon
, p. 4069 - 4080 (2019/08/26)
Translocator protein (TSPO) expression is closely related with neuroinflammation and neuronal damage which might cause several central nervous system diseases. Herein, a series of TSPO ligands (11a–c and 13a–d) with a 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamide structure were prepared and evaluated via an in vitro binding assay. Most of the novel ligands exhibited a nano-molar affinity for TSPO, which was better than that of DPA-714. Particularly, 11a exhibited a subnano-molar TSPO binding affinity with suitable lipophilicity for in vivo brain studies. After radiolabeling with fluorine-18, [18F]11a was used for a dynamic positron emission tomography (PET) study in a rat LPS-induced neuroinflammation model; the inflammatory lesion was clearly visualized with a superior target-to-background ratio compared to [18F]DPA-714. An immunohistochemical examination of the dissected brains confirmed that the uptake location of [18F]11a in the PET study was consistent with a positively activated microglia region. This study proved that [18F]11a could be employed as a potential PET tracer for detecting neuroinflammation and could give possibility for diagnosis of other diseases, such as cancers related with TSPO expression.