Radiosynthesis, photoisomerization, biodistribution, and metabolite analysis of 11C-PBB3 as a clinically useful PET probe for imaging of tau pathology

H Hashimoto, K Kawamura, N Igarashi… - Journal of Nuclear …, 2014 - Soc Nuclear Med
2-((1 E, 3 E)-4-(6-(11C-methylamino) pyridin-3-yl) buta-1, 3-dienyl) benzo [d] thiazol-6-ol
(11C-PBB3) is a clinically useful PET probe that we developed for in vivo imaging of tau …

Identification of a major radiometabolite of [11C] PBB3

H Hashimoto, K Kawamura, M Takei, N Igarashi… - Nuclear medicine and …, 2015 - Elsevier
Abstract Introduction [11 C] PBB3 is a clinically used positron emission tomography (PET)
probe for in vivo imaging of tau pathology in the brain. Our previous study showed that [11 C] …

PET quantification of tau pathology in human brain with 11C-PBB3

Y Kimura, M Ichise, H Ito, H Shimada… - Journal of Nuclear …, 2015 - Soc Nuclear Med
Tau accumulation in the brain is a pathologic hallmark of Alzheimer disease and other
tauopathies. Quantitative visualization of tau pathology in humans can be a powerful method …

Radiosynthesis, In Vitro and In Vivo Evaluation of [18F]CBD-2115 as a First-in-Class Radiotracer for Imaging 4R-Tauopathies

A Lindberg, AC Knight, D Sohn, L Rakos… - ACS chemical …, 2021 - ACS Publications
CBD-2115 was selected from a library of 148 compounds based on a pyridinyl-indole
scaffold as a first-in-class 4R-tau radiotracer. In vitro binding assays showed [3H] CBD-2115 …

[HTML][HTML] Characterization of 18F-PM-PBB3 (18F-APN-1607) Uptake in the rTg4510 Mouse Model of Tauopathy

CC Weng, IT Hsiao, QF Yang, CH Yao, CY Tai, MF Wu… - Molecules, 2020 - mdpi.com
Misfolding, aggregation, and cerebral accumulation of tau deposits are hallmark features of
Alzheimer's disease. Positron emission tomography study of tau can facilitate the …

Preclinical evaluation of 18F-JNJ64349311, a novel PET tracer for tau imaging

L Declercq, F Rombouts, M Koole… - Journal of nuclear …, 2017 - Soc Nuclear Med
In this study, we have synthesized and evaluated 18F-JNJ64349311, a tracer with high
affinity for aggregated tau (inhibition constant value, 8 nM) and high (≥ 500×) in vitro …

Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease

N Okamura, S Furumoto, R Harada… - Journal of Nuclear …, 2013 - Soc Nuclear Med
Neurofibrillary tangles in Alzheimer disease (AD) brains are composed of the microtubule-
associated protein tau. Noninvasive monitoring of tau protein aggregates in the living brain …

[HTML][HTML] Dual tracer tau PET imaging reveals different molecular targets for 11C-THK5351 and 11C-PBB3 in the Alzheimer brain

K Chiotis, P Stenkrona, O Almkvist, V Stepanov… - European Journal of …, 2018 - Springer
Purpose Several tau PET tracers have been developed, but it remains unclear whether they
bind to the same molecular target on the heterogeneous tau pathology. In this study we …

Preclinical evaluation of 18F-RO6958948, 11C-RO6931643, and 11C-RO6924963 as novel PET radiotracers for imaging tau aggregates in Alzheimer disease

M Honer, L Gobbi, H Knust, H Kuwabara… - Journal of Nuclear …, 2018 - Soc Nuclear Med
Tau aggregates and amyloid-β (Aβ) plaques are key histopathologic features in Alzheimer
disease (AD) and are considered targets for therapeutic intervention as well as biomarkers …

Characterization of 3 novel tau radiopharmaceuticals, 11C-RO-963, 11C-RO-643, and 18F-RO-948, in healthy controls and in Alzheimer subjects

DF Wong, RA Comley, H Kuwabara… - Journal of Nuclear …, 2018 - Soc Nuclear Med
11C-RO-963, 11C-RO-643, and 18F-RO-948 (previously referred to as 11C-RO6924963,
11C-RO6931643, and 18F-RO6958948, respectively) have been reported as promising PET …