[<sup>18</sup>F]TRACK, a PET tracer for imaging of tropomyosin receptor kinases (Trk): Efficient radiosynthesis and preliminary evaluation in the TgF344‐AD rat model of Alzheimer’s disease
نویسندگان
چکیده
Background A family of tropomyosin receptor kinases (TrkA/B/C) plays important roles in the regulation neuronal differentiation, growth, and survival via their interactions with neurotrophins. growing body literature suggests downregulation Trk many neurodegenerative conditions central nervous system (CNS), including Alzheimer’s disease (AD). We recently reported development [18F]TRACK, PET tracers for vivo imaging TrkB its first in-human study. Here, we wish to report a fully automated GMP-compliant radiosynthesis [18F]TRACK at high radiochemical purity (RCP) molar activity preliminary evaluation wild-type transgenic rat model AD. Method Radiosynthesis was performed using Scintomics GRP module copper-catalyzed 18F-fluorination chiral boron pinacolate precursor. Brain (n = 3) TgF344-AD models 2) 23 months on microPET Concord R4 scanner. Result synthesized 5.0±1.4% yield not corrected decay (activity range 95-154 mCi) >99% RCP activities 250 ± 75 GBq/µmol 6). The synthesis all batches passed quality control procedures, chemical purity, sterility pyrogenicity. tracer showed moderate brain uptake rats highest accumulation thalamus (SUVmax 1.56 0.28, 10 min post-injection), consistent regional distribution humans acquired parallel Preliminary data lower AD thalamus, striatum frontal cortex compared animals. Conclusion This study demonstrated feasibility production sufficient doses scanning multiple subjects per day or long deliveries. biodistribution studies preferential across species. These findings warrants further expression implication psychiatric pathologies [18F]TRACK.
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ژورنال
عنوان ژورنال: Alzheimers & Dementia
سال: 2023
ISSN: ['1552-5260', '1552-5279']
DOI: https://doi.org/10.1002/alz.065138