1015460-59-9Relevant articles and documents
An one-pot two-step automated synthesis of [18F]T807 injection, its biodistribution in mice and monkeys, and a preliminary study in humans
Huang, Ya-Yao,Chiu, Ming-Jang,Yen, Ruoh-Fang,Tsai, Chia-Ling,Hsieh, Hao-Yu,Chiu, Ching-Hung,Wu, Chi-Han,Hsin, Ling-Wei,Tzen, Kai-Yuan,Cheng, Cheng-Yi,Ma, Kuo-Hsing,Shiue, Chyng-Yann
, (2019)
[18F]T807 is a potent tau protein imaging agent. In order to fulfill the demand from preclinical and clinical studies, we developed an automated one-pot two-step synthesis of this potent tau imaging agent and studied its stability, and dosimetr
PI-2620 Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer's Disease and Other Tauopathies
Berndt, Mathias,Capotosti, Francesca,Dinkelborg, Ludger,Gabellieri, Emanuele,Hickman, David,Kroth, Heiko,Molette, Jerome,Mueller, Andre,Oden, Felix,Pfeifer, Andrea,Schieferstein, Hanno,Schmitt-Willich, Heribert,Serra, Andreia Monica,Sreenivasachary, Nampally,Stephens, Andrew
, p. 12808 - 12830 (2021/09/13)
The first candidate PI-2014 was tested in healthy controls and subjects with Alzheimer's disease (AD). As PI-2014 displayed off-target binding to monoamine oxidase A (MAO-A), a new lead with improved binding to Tau and decreased MAO-A binding was required. For compound optimization, Tau binding assays based on both human AD brain homogenate and Tau-paired helical filaments were employed. Furthermore, two MAO-A screening assays based on (1) human-recombinant MAO-A and (2) displacement of 2-fluoro-ethyl-harmine from mouse brain homogenate were employed. Removing the N-methyl group from the tricyclic core resulted in compounds displaying improved Tau binding. For the final round of optimization, the cyclic amine substituents were replaced by pyridine derivatives. PI-2620 (2-(2-fluoropyridin-4-yl)-9H-pyrrolo[2,3-b:4,5-c′]dipyridine) emerged as a best candidate displaying high Tau binding, low MAO-A binding, high brain uptake, and fast and complete brain washout. Furthermore, PI-2620 showed Tau binding on brain sections from corticobasal degeneration, progressive supranuclear palsy, and Pick's disease.
Novel compounds useful as fluorescent probes selectively binding to tau aggregates and preparation method thereof
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, (2021/01/29)
A compound having high selectivity for tau aggregates and a method for preparing the same. The present invention relates to a tau targeting fluorescent probe including the compound, a composition for detecting tau fiber protein comprising the fluorescent