24330-53-8Relevant articles and documents
High-Field Proton and Carbon-13 Nuclear Magnetic Resonance Studies of the Conformational Dynamic Properties of Seven-Membered Rings. 3-Substituted Derivatives of 1,5-Benzodioxepin
Menard, D.,St-Jacques, M.
, p. 2055 - 2063 (1984)
The conformational and dynamic properties of the 3-methyl (6), 3-methoxy (7), and 3-methoxy-3-methyl (8) derivatives of 1,5-benzodioxepin 1 have been investigated by high-field 1H and 13C NMR methods.Analyses of the spectra at low temperatures (below coal
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.
Novel potential pyrazolopyrimidine based translocator protein ligands for the evaluation of neuroinflammation with PET
Kwon, Young-Do,Kang, Shinwoo,Park, Hyunjun,Cheong, Il-koo,Chang, Keun-A,Lee, Sang-Yoon,Jung, Jae Ho,Lee, Byung Chul,Lim, Seok Tae,Kim, Hee-Kwon
, p. 292 - 306 (2018/10/15)
Translocator protein (TSPO) is an interesting biological target because TSPO overexpression is associated with microglial activation caused by neuronal damage or neuroinflammation, and these activated microglia are involved in several central nervous syst