Selective α-Synuclein PET Radiotracer Development- Characterization

IF 1 4区 医学 Q4 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Nuklearmedizin-nuclear Medicine Pub Date : 2023-03-30 DOI:10.1055/s-0043-1766158
B. Hooshyar Yousefi, B. C. Uzuegbunam, W. Paslawski, G. B. Kotipalli, M. Luster, D. Librizzi, W. Weber, P. Svenningsson, T. Arzberger
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Abstract

Ziel/Aim The deposition of α-synuclein fibrils (α-syn) is a major feature that unites a group of neurodegenerative diseases collectively known as the synucleinopathies. Presently, the in vivo detection of this biomarker is not possible due to lack of suitable radiotracers. Scientists from academics and industry are interested to develop radiotracers for the early diagnosis of α-synucleinopathies. Disarylbisthiazoles (DABTAs) based ligands have been showing high affinity towards α-syn and excellent selectivity over tau and Aβ aggregates. The aim of this work is characterization of the radiotracers within competition binding assays, autoradiography and pharmacokinetics (PK) study to confirm their high binding affinity and optimized pharmacokinetics and utilize them as a promising α-syn PET tracer.
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选择性α-突触核蛋白PET示踪剂的研制与表征
α-突触核蛋白原纤维(α-syn)的沉积是联合一组神经退行性疾病(统称为突触核蛋白病)的主要特征。目前,由于缺乏合适的放射性示踪剂,这种生物标志物的体内检测是不可能的。学术界和工业界的科学家对开发用于α-突触核蛋白病早期诊断的放射性示踪剂很感兴趣。基于二芳基双噻唑(DABTAs)的配体对α-syn具有高亲和力,对tau和a - β聚集物具有良好的选择性。本研究的目的是在竞争结合分析、放射自显影和药代动力学(PK)研究中对放射性示踪剂进行表征,以证实其高结合亲和力和优化的药代动力学,并将其作为一种有前景的α-syn PET示踪剂。
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来源期刊
CiteScore
1.70
自引率
13.30%
发文量
267
审稿时长
>12 weeks
期刊介绍: Als Standes- und Fachorgan (Organ von Deutscher Gesellschaft für Nuklearmedizin (DGN), Österreichischer Gesellschaft für Nuklearmedizin und Molekulare Bildgebung (ÖGN), Schweizerischer Gesellschaft für Nuklearmedizin (SGNM, SSNM)) von hohem wissenschaftlichen Anspruch befasst sich die CME-zertifizierte Nuklearmedizin/ NuclearMedicine mit Diagnostik und Therapie in der Nuklearmedizin und dem Strahlenschutz: Originalien, Übersichtsarbeiten, Referate und Kongressberichte stellen aktuelle Themen der Diagnose und Therapie dar. Ausführliche Berichte aus den DGN-Arbeitskreisen, Nachrichten aus Forschung und Industrie sowie Beschreibungen innovativer technischer Geräte, Einrichtungen und Systeme runden das Konzept ab. Die Abstracts der Jahrestagungen dreier europäischer Fachgesellschaften sind Bestandteil der Kongressausgaben. Nuklearmedizin erscheint regelmäßig mit sechs Ausgaben pro Jahr und richtet sich vor allem an Nuklearmediziner, Radiologen, Strahlentherapeuten, Medizinphysiker und Radiopharmazeuten.
期刊最新文献
The Medical Informatics Initiative and the Network University Medicine - Perspectives for Nuclear Medicine. Combined morphologic-metabolic biomarkers from [18F]FDG-PET/CT stratify prognostic groups in low-risk NSCLC. NuklearMedizin 2024: Abstract-Einreichung bis zum 1. November geöffnet! DGN-Forschungs- und -Förderpreise Preisverleihungen
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