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

CRANAD-102 is a highly promising, near-infrared fluorescence-based tracer with 68-fold selectivity for soluble oligomeric forms of amyloid β over its aggregates. This work describes the radiosynthesis of carbon-11-labeled CRANAD-102 via a Suzuki–Miyaura reaction in an RCС of 48 ± 9%, with an RCP of>96% and a molar activity of 25  ± 7 GBq/μmol. 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 s pecies of Aβ in humans. These soluble and protofibrillar species are thought to be responsible to cause AD. Within this work, we successfully11C-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.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research