Positron Emission Tomography (PET) imaging agents for Alzheimer’s Disease currently utilize 11C or 18F radionuclides, the incorporation methods and short half-lives of which make difficult their widespread clinical use. We have sought to create ligands suitable for complexation with Cu-64 to serve as alternative PET imaging agents for AD with longer half-lives and easier methods of radionuclide incorporation. Modification of a triazacyclonone (TACN) backbone by variations in the N-linked fragments allows for ‘tuning’ of several ligand properties. Ligand tuning via two mechanisms has been explored: the number of amyloid-targeting fragments and the size of aliphatic substituents. By varying the number of amyloid-targeting fragments, the beneficial effect of incorporating a second amyloid-targeting fragment to increase affinity for amyloid plaques is weighed against the drawback of ligand size. By varying the size of the aliphatic substituent, the benefit of increased aliphatic nature of the ligand can be measured and weighed against the drawback of increased bulk close to the Cu-chelating pocket of the ligand. Physical and in vivo characterization of the derivatized ligands has allowed for determination of the PET imaging potential of the ligands in relation to the ‘tuning’ of their physical structure

Ligand tuning for 64cu Positron Emission Tomography (PET) imaging in alzheimer's disease

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