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- 横山 裕香
- 東北大・院医・機能薬理学分野
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- 原田 龍一
- 東北大・院医・機能薬理学分野
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- Pradith Lerdsirisuk
- 東北大・サイクロトロンRIセンター・核薬学研究部
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- 清水 悠暉
- 東北大・サイクロトロンRIセンター・核薬学研究部
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- 堵 怡青
- 東北大・院医・機能薬理学分野
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- 石川 洋一
- 東北大・サイクロトロンRIセンター・核薬学研究部
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- 荒井 啓行
- 東北大・加齢医学研究所・認知症治療医薬開発寄附研究部門
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- 工藤 幸司
- 東北大・加齢医学研究所・認知症治療医薬開発寄附研究部門
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- 古本 祥三
- 東北大・サイクロトロンRIセンター・核薬学研究部
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- 岡村 信行
- 東北医科薬科大・医・薬理
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- 谷内 一彦
- 東北大・院医・機能薬理学分野
書誌事項
- タイトル別名
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- Comparison of the binding characteristics of [¹⁸F]SNFT-1 and other tau imaging tracers to Alzheimer's disease pathology
抄録
<p>Introduction: Misfolded tau aggregates associated with clinical syndromes and various neurodegenerative diseases. To date, many second-generation of tau PET tracers were developed to overcome the limitation of the first-generation such as off-target binding. Recently, we developed [¹⁸F]SNFT-1 from compound optimization of [¹⁸F]THK-5351, which showed high affinity for monoamine oxidase-B (MAO-B) as off-target binding. The aim of study was to compare the binding properties of [¹⁸F]SNFT-1 and second-generation tau PET radiotracers to human brain tissues.</p><p>Methods: In vitro competitive binding assay were performed for tau aggregates, amyloid aggregates, and recombinant MAO-A and MAO-B. After preparing 18F-labeled compounds, in vitro autoradiography was performed using frozen human brain sections with immunostaining of phosphorylated tau (tau IHC) for evaluation of binding selectivity.</p><p>Results and Discussion: Although second-generation of tau PET radiotracers showed a similar binding affinity for tau aggregates, the off-target binding affinity was different. SNFT-1 showed a high binding affinity for tau aggregates, which was comparable to MK-6240, with no interaction of amyloid aggregates as well as MAO enzymes. In vitro autoradiography demonstrated that distribution of radiotracer's binding was similar to tau IHC in the medial temporal area of Alzheimer's disease. On the other hands, second-generation tau PET radiotracers showed little binding to the frontal cortex in a case of progressive supranuclear palsy that contains high density tau aggregates. </p><p>Conclusion: [18F]SNFT-1 would be a promising candidates for imaging tau aggregates. Further binding characterization is required to validate the binding of non-AD tau aggregates.</p>
収録刊行物
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- 日本薬理学会年会要旨集
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日本薬理学会年会要旨集 95 (0), 1-SS-45-, 2022
公益社団法人 日本薬理学会
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詳細情報 詳細情報について
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- CRID
- 1390573242665295360
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- ISSN
- 24354953
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- 本文言語コード
- ja
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- データソース種別
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- JaLC
- Crossref
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- 抄録ライセンスフラグ
- 使用不可