A gallium fluoride-18 complex containing a pentadentate macrocyclic ligand with a dimethylaminostilbene functional group designed for diagnostic imaging of Alzheimer's disease
Journal Title
Dalton Transactions
Publication Type
Online publication before print
Abstract
The molecular pathology of Alzheimer's disease is associated with the presence of aggregates of amyloid-β, a 39-43 amino acid peptide, that form amyloid plaques in the brain. Appropriately substituted stilbene derivatives, radiolabelled with positron-emitting radionuclides, that bind selectively to amyloid-β plaques can be used to assess plaque burden by Positron Emission Tomography (PET) imaging and assist in the diagnosis of Alzheimer's disease. In this work, a substituted pentadentate ligand based on a triazacyclononane backbone (H(2)L(1)) with one pendent stilbene functional group and two pendent carboxylate groups was synthesised. The new ligand binds to amyloid-β plaques present in human brain tissue. Non-conventional radiolabelling with fluorine-18 was achieved by the formation of a Ga(III)-[(18)F]F(-) coordinate bond to give a complex, [(18)F][GaL(1)F]. This ligand can also be radiolabelled with gallium-68 to give [(68)Ga][GaL(1)F], or copper-64 to give [(64)Cu][CuL(1)]. The in vivo biodistribution of [(18)F][GaL(1)F] and [(64)Cu][CuL(1)] was evaluated in mice, revealing that the initial uptake of [(18)F][GaL(1)F] and [(64)Cu][CuL(1)] in the brain was 0.85 ± 0.13% IA g(-1) and 0.71 ± 0.03% IA g(-1) respectively. An increase in radioactivity in bone at later time points suggested that [(18)F][GaL(1)F] is unstable in vivo.
Department(s)
Cancer Imaging; Laboratory Research
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