Development of 11C-labeled CRANAD-102 for positron emission tomography imaging of soluble Aβ-species

Abstract

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.