Markus Staudt, Vladimir Shalgunov, Maiken Nedergaard, Matthias M. Herth
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Development of 11C-labeled CRANAD-102 for positron emission tomography imaging of soluble Aβ-species
CRANAD-102, a selective near-infrared fluorescent tracer targeting soluble amyloid-β (Aβ) species, has recently attracted attention due to its potential to be used as a diagnostic tool for early stages of Alzheimer's disease (AD). Development of a positron emission tomography (PET) tracer based on CRANAD-102 could as such allow to noninvasively study soluble and protofibrillar species of Aβ in humans. These soluble and protofibrillar species are thought to be responsible to cause AD. Within this work, we successfully 11C-labeled CRANAD-102 via a Suzuki–Miyaura reaction in a RCС of 48 ± 9%, with a RCP of >96% and a molar activity (Am) of 25 ± 7 GBq/μmol. Future studies have to be conducted to evaluate if [11C]CRANAD-102 can be used to detect soluble protofibrils in vivo and if [11C]CRANAD-102 can be used to detect AD earlier as possible with current diagnostics.
期刊介绍：
The Journal of Labelled Compounds and Radiopharmaceuticals publishes all aspects of research dealing with labeled compound preparation and applications of these compounds. This includes tracer methods used in medical, pharmacological, biological, biochemical and chemical research in vitro and in vivo.
The Journal of Labelled Compounds and Radiopharmaceuticals devotes particular attention to biomedical research, diagnostic and therapeutic applications of radiopharmaceuticals, covering all stages of development from basic metabolic research and technological development to preclinical and clinical studies based on physically and chemically well characterized molecular structures, coordination compounds and nano-particles.
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