The deposition of β-amyloid (Aβ) in the brain
is a
pathologic hallmark of Alzheimer’s disease (AD), appearing
years before the onset of symptoms, and its detection is incorporated
into clinical diagnosis. Here, we have discovered and developed a
class of diaryl-azine derivatives for detecting Aβ plaques in
the AD brain using PET imaging. After a set of comprehensive preclinical
assessments, we screened out a promising Aβ-PET tracer, [18F]92, with a high binding affinity to the Aβ
aggregates, significant binding ability with the AD brain sections,
and optimal brain pharmacokinetic properties in rodents and non-human
primates. The first-in-human PET study declared that [18F]92 displayed low white matter uptake and could bind
to Aβ pathology for distinguishing AD from healthy control subjects.
All these results support that [18F]92 might
become a promising PET tracer for visualizing Aβ pathology in
AD patients.
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