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Issue 5, 2013
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Radiosynthesis and characterization of astemizole derivatives as lead compounds toward PET imaging of τ-pathology

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Abstract

Formation of neurofibrillary tangles, comprising of microtubule-associated tau protein, is a hallmark of a group of neurodegenerative diseases, including Alzheimer's disease. In consequence, in vivo imaging of neurofibrillary tangles is a current focus of positron emission tomography research. Herein, development of an in vitro radioligand binding assay which uses synthetic aggregates as a model of neurofibrillary tangles is reported, together with evaluation of novel derivatives of the tau protein ligand astemizole.

Graphical abstract: Radiosynthesis and characterization of astemizole derivatives as lead compounds toward PET imaging of τ-pathology

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The article was received on 14 Jan 2013, accepted on 13 Mar 2013 and first published on 14 Mar 2013


Article type: Concise Article
DOI: 10.1039/C3MD00017F
Med. Chem. Commun., 2013,4, 852-855

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    Radiosynthesis and characterization of astemizole derivatives as lead compounds toward PET imaging of τ-pathology

    P. J. Riss, L. Brichard, V. Ferrari, D. J. Williamson, T. D. Fryer, Y. T. Hong, J. Baron and F. I. Aigbirhio, Med. Chem. Commun., 2013, 4, 852
    DOI: 10.1039/C3MD00017F

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