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(68)Ga-Labeled Benzothiazole Derivatives for Imaging Aβ Plaques in Cerebral Amyloid Angiopathy
[Image: see text] Timely diagnostic imaging plays a crucial role in managing cerebral amyloid angiopathy (CAA)—the condition in which amyloid β is deposited on blood vessels. To selectively map these amyloid plaques, we have designed amyloid-targeting ligands that can effectively complex with (68)Ga...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9202065/ https://www.ncbi.nlm.nih.gov/pubmed/35721913 http://dx.doi.org/10.1021/acsomega.2c02369 |
Sumario: | [Image: see text] Timely diagnostic imaging plays a crucial role in managing cerebral amyloid angiopathy (CAA)—the condition in which amyloid β is deposited on blood vessels. To selectively map these amyloid plaques, we have designed amyloid-targeting ligands that can effectively complex with (68)Ga(3+) while maintaining good affinity for amyloid β. In this study, we introduced novel 1,4,7-triazacyclononane-based bifunctional chelators (BFCs) that incorporate a benzothiazole moiety as the Aβ-binding fragment and form charged and neutral species with (68)Ga(3+). In vitro autoradiography using 5xFAD and WT mouse brain sections (11-month-old) suggested strong and specific binding of the (68)Ga complexes to amyloid β. Biodistribution studies in CD-1 mice revealed a low brain uptake of 0.10–0.33% ID/g, thus suggesting (68)Ga-labeled novel BFCs as promising candidates for detecting CAA. |
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