Issue 5, 2013
From the journal:

MedChemComm

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

Patrick J. Riss,*abc   Laurent Brichard,a   Valentina Ferrari,a   David J. Williamson,a   Tim D. Fryer,ab   Young T. Hong,a   Jean-Claude Barona  and  Franklin I. Aigbirhioab  

* Corresponding authors

a Wolfson Brain Imaging Centre, University of Cambridge, Addenbrooke's Hospital, Cambridge, UK
E-mail: pr340@wbic.cam.ac.uk
Fax: +44 (0)1223 331826
Tel: +44 (0)1223 331823

b Behavioural and Clinical Neuroscience Institute, University of Cambridge, Cambridge, UK

c Department of Chemistry, Universitetet i Oslo, Postboks 1033, Blindern, Oslo, Norge
E-mail: Patrick.Riss@kjemi.uio.no
Tel: +47 228 57673

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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Article information

DOI
https://doi.org/10.1039/C3MD00017F
Article type
Concise Article
Submitted
14 Jan 2013
Accepted
13 Mar 2013
First published
14 Mar 2013

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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