Synthesis and evaluation of novel potent TSPO PET ligands with 2-phenylpyrazolo [1,5-a]pyrimidin-3-yl acetamide
DC Field | Value | Language |
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dc.contributor.author | Van Hieu Tran | - |
dc.contributor.author | Park, Hyunjun | - |
dc.contributor.author | Park, Jaekyung | - |
dc.contributor.author | Kwon, Young-Do | - |
dc.contributor.author | Kang, Shinwoo | - |
dc.contributor.author | Jung, Jae Ho | - |
dc.contributor.author | Chang, Keun-A | - |
dc.contributor.author | Lee, Byung Chul | - |
dc.contributor.author | Lee, Sang-Yoon | - |
dc.contributor.author | Kang, Soosung | - |
dc.contributor.author | Kim, Hee-Kwon | - |
dc.date.available | 2020-02-27T02:22:20Z | - |
dc.date.created | 2020-02-04 | - |
dc.date.issued | 2019-09-15 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/1009 | - |
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 | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.subject | PERIPHERAL BENZODIAZEPINE-RECEPTOR | - |
dc.subject | PROTEIN 18 KDA | - |
dc.subject | TRANSLOCATOR PROTEIN | - |
dc.subject | BIOLOGICAL EVALUATION | - |
dc.subject | INITIAL EVALUATION | - |
dc.subject | F-18 | - |
dc.subject | DPA-714 | - |
dc.subject | NEUROINFLAMMATION | - |
dc.subject | RADIOLIGANDS | - |
dc.subject | MICROGLIA | - |
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.type.rims | ART | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000482845600009 | - |
dc.identifier.doi | 10.1016/j.bmc.2019.07.036 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY, v.27, no.18, pp.4069 - 4080 | - |
dc.identifier.scopusid | 2-s2.0-85071007065 | - |
dc.citation.endPage | 4080 | - |
dc.citation.startPage | 4069 | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.citation.volume | 27 | - |
dc.citation.number | 18 | - |
dc.contributor.affiliatedAuthor | Park, Hyunjun | - |
dc.contributor.affiliatedAuthor | Park, Jaekyung | - |
dc.contributor.affiliatedAuthor | Kang, Shinwoo | - |
dc.contributor.affiliatedAuthor | Chang, Keun-A | - |
dc.contributor.affiliatedAuthor | Lee, Sang-Yoon | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | Translocator protein | - |
dc.subject.keywordAuthor | Positron emission tomography probe | - |
dc.subject.keywordAuthor | Structure activity relationships | - |
dc.subject.keywordAuthor | Neuroinflammation | - |
dc.subject.keywordPlus | PERIPHERAL BENZODIAZEPINE-RECEPTOR | - |
dc.subject.keywordPlus | PROTEIN 18 KDA | - |
dc.subject.keywordPlus | TRANSLOCATOR PROTEIN | - |
dc.subject.keywordPlus | BIOLOGICAL EVALUATION | - |
dc.subject.keywordPlus | INITIAL EVALUATION | - |
dc.subject.keywordPlus | F-18 | - |
dc.subject.keywordPlus | DPA-714 | - |
dc.subject.keywordPlus | NEUROINFLAMMATION | - |
dc.subject.keywordPlus | RADIOLIGANDS | - |
dc.subject.keywordPlus | MICROGLIA | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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