11C-labeled stilbene derivatives as Aβ-aggregate-specific PET imaging agents for Alzheimer’s disease

Synthesis of a PET tau tracer [11C]PBB3 for imaging of Alzheimer’s disease

“…The original radiosynthesis of [ 11 C]PIB utilized the hydroxyl group protected precursor for carbon-11 labeling at amino group, followed by deprotection. 46 Later a rapid one-step radiosynthesis of [ 11 C]PIB using unprotected precursor for direct radiolabeling was developed, 47,48 which has become a popular radiosynthesis method for 11 C]6 in 20-25% decay-corrected radiochemical yield. This is a 1-pot-1-step radiosynthesis with higher radiochemical yield and shorter overall synthesis time.…”

Development of Positron-Emission Tomography/Single-Photon Emission Computed Tomography Imaging Probes for in Vivo Detection of .BETA.-Amyloid Plaques in Alzheimer's Brains

“…Taken together, the data strongly suggest that the new 11 C-labeled stilbene compound, [ 11 C]4, may be a useful PET tracer for imaging Ab plaques in the brain of patients with AD. 9) In an attempt to develop more useful Ab-specific imaging agents, we investigated a novel series of benzofuran derivatives, designed to be isosteric analogues of thioflavin-T (ThT) (Fig. 3).…”

“…However, the in vivo nonspecific binding of these probes, as reflected by their slow washout from the normal mouse brain, made them unsuitable for in vivo Ab 26) These previous findings suggested that additional structural changes to these benzofurans may lead to the development of useful amyloid-specific imaging agents. Then, we designed and synthesized a new series of benzofuran derivatives (7)(8)(9)(10)(11)(12) Next, compound 10 was investigated for its neuropathologic staining of SPs in human AD brain sections (Fig. 4).…”

18F-Labeled Phenyldiazenyl Benzothiazole for in Vivo Imaging of Neurofibrillary Tangles in Alzheimer's Disease Brains

“…Therefore, considerable effort has focused on the development of imaging probes targeting SPs for positron emission tomography (PET) and single photon emission computed tomography (SPECT). Among them, PET/SPECT probes such as IMPY, 2 SB-13, 3 PIB, 4 AZD2184, 5 FDDNP, 6 BAY94-9172, 7 AV-45, 8 and GE-067 9 have been tested clinically and demonstrated the potential utility of the in vivo imaging of SPs in the brain. Many other compounds with structural similarities have also been reported.…”