[Development of SPECT Probes for In Vivo Imaging of β-Amyloid and Tau Aggregates in the Alzheimer's Disease Brain].

In this study, we designed and synthesized novel Aβ and tau imaging probes for SPECT. [(125)I]PBOX-3, developed as an Aβ imaging probe, showed high affinity for Aβ aggregates in vitro. A SPECT/CT study with [(123)I]PBOX-3 revealed a higher level of radioactivity in a Tg2576 mouse, which is the AD model mouse, than in a wild-type mouse. In addition, ex vivo autoradiograms of brain sections from a Tg2576 mouse after the injection of [(123)I]PBOX-3 showed the selective binding of Aβ plaques. BIP-NMe2, developed as a tau imaging probe, showed high and selective affinity for tau aggregates in AD brain sections. In addition, [(125)I]BIP-NMe2 displayed high initial uptake into, and fast washout from, the normal mouse brain, suggesting that [(125)I]BIP-NMe2 has favorable pharmacokinetics for the in vivo imaging of tau aggregates. Taken together, we successfully developed an Aβ imaging probe, PBOX-3, and a tau imaging probe, BIP-NMe2. These probes may be used to develop novel methods for the diagnosis, treatment and monitoring of AD progression. PMID: 29093372 [PubMed - in process]
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - Category: Drugs & Pharmacology Authors: Tags: Yakugaku Zasshi Source Type: research