18F-barbiturates are PET tracers with diagnostic potential in Alzheimer's disease

Elisa Calamai; Sergio Dall'Angelo; David Koss; Juozas Domarkas; Timothy J. McCarthy; Marco Mingarelli; Gernot Riedel; Lutz F. Schweiger; Andy Welch; Bettina Platt; Matteo Zanda

doi:10.1039/C2CC38443D

¹⁸F-barbiturates are PET tracers with diagnostic potential in Alzheimer's disease†

Elisa Calamai,^a Sergio Dall'Angelo,^a David Koss,^a Juozas Domarkas,^a Timothy J. McCarthy,^b Marco Mingarelli,^a Gernot Riedel,^a Lutz F. Schweiger,^a Andy Welch,^a Bettina Platt*^a and Matteo Zanda*^a

Author affiliations

* Corresponding authors

^a Kosterlitz Centre for Therapeutics, Institute of Medical Sciences and J. Mallard Scottish PET Centre, University of Aberdeen, Foresterhill, Scotland, UK
E-mail: m.zanda@abdn.ac.uk, b.platt@abdn.ac.uk

^b Precision Medicine, Pfizer WRD, Groton, CT, USA

Abstract

Three fluoro-barbiturates were synthesised, showing in vivo sedative efficacy. One of them, [¹⁸F]1a, was synthesised in radiofluorinated form. PET/CT Imaging with [¹⁸F]1a identified β-amyloid over-expressing transgenic mice (βA mice) compared to wild type and tau lines. The fluorescent barbiturate 9 was able to label βA plaques in brain sections of βA mice, and co-localise with a fluorescent Zn(II) indicator.

Chemical Communications

¹⁸F-barbiturates are PET tracers with diagnostic potential in Alzheimer's disease†

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¹⁸F-barbiturates are PET tracers with diagnostic potential in Alzheimer's disease

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