Structural characteristics |
18F-labelled PBB derivatives |
|
Pyridine isoquinoline amine derivative |
|
|
Preclinical study |
-Higher signal-to-background ratio |
-Rapid pharmacokinetics |
-High affinity |
-High affinity |
-High affinity |
-Less off-target signals than [11C]PBB3 |
-No off-target binding to MAO-A /MAO-B |
-High selectivity over Aβ, MAO-A and MAO-B |
-High selectivity over Aβ, MAO-A and MAO-B |
-Low off-target binding |
Clinical Human study |
-Broader dynamic range compared to [11C]PBB3 |
-Favourable pharmacokinetics |
-No off-target binding in regions seen in first-generation tau tracers |
-Favourable pharmacokinetics |
-No prominent off-target binding in the basal ganglia and thalamus |
-Correlated well with neuropathological staging of NFTs |
-High affinity |
-No off-target binding in the basal ganglia and choroid plexus |
-High selectivity over Aβ, MAO-A and MAO-B |
-Mild tracer retention in the substantia nigra and meninges |
-High signal-to-background ratio |
References |
[66•] |
[56•] |
[57•, 59, 60] |
[62] |
[63, 65•, 67] |