Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 강수성 | * |
dc.date.accessioned | 2019-10-02T02:00:03Z | - |
dc.date.available | 2019-10-02T02:00:03Z | - |
dc.date.issued | 2019 | * |
dc.identifier.issn | 0968-0896 | * |
dc.identifier.issn | 1464-3391 | * |
dc.identifier.other | OAK-25365 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/251499 | - |
dc.description.abstract | 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, [F-18] 11a Filla 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 [F-18]DPA-714. An immunohistochemical examination of the dissected brains confirmed that the uptake location of [F-18] 11a in the PET study was consistent with a positively activated microglia region. This study proved that [F-18] 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. | * |
dc.language | English | * |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | * |
dc.subject | Translocator protein | * |
dc.subject | Positron emission tomography probe | * |
dc.subject | Structure activity relationships | * |
dc.subject | Neuroinflammation | * |
dc.title | Synthesis and evaluation of novel potent TSPO PET ligands with 2-phenylpyrazolo [1,5-a]pyrimidin-3-yl acetamide | * |
dc.type | Article | * |
dc.relation.issue | 18 | * |
dc.relation.volume | 27 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 4069 | * |
dc.relation.lastpage | 4080 | * |
dc.relation.journaltitle | BIOORGANIC & MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1016/j.bmc.2019.07.036 | * |
dc.identifier.wosid | WOS:000482845600009 | * |
dc.identifier.scopusid | 2-s2.0-85071007065 | * |
dc.author.google | Van Hieu Tran | * |
dc.author.google | Park, Hyunjun | * |
dc.author.google | Park, Jaekyung | * |
dc.author.google | Kwon, Young-Do | * |
dc.author.google | Kang, Shinwoo | * |
dc.author.google | Jung, Jae Ho | * |
dc.author.google | Chang, Keun-A | * |
dc.author.google | Lee, Byung Chul | * |
dc.author.google | Lee, Sang-Yoon | * |
dc.author.google | Kang, Soosung | * |
dc.author.google | Kim, Hee-Kwon | * |
dc.contributor.scopusid | 강수성(56177300500) | * |
dc.date.modifydate | 20240301081003 | * |