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Issue 6, 2015
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Synthesis and evaluation of [11C]PBD150, a radiolabeled glutaminyl cyclase inhibitor for the potential detection of Alzheimer's disease prior to amyloid β aggregation

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Abstract

The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci μmol−1, n = 5). Evaluation of [11C]PBD150 by small animal PET imaging (mouse and rat) determined it does not permeate the blood brain barrier, indicating previously described therapeutic effect in transgenic mice was likely not the result of inhibiting central nervous system glutaminyl cyclase.

Graphical abstract: Synthesis and evaluation of [11C]PBD150, a radiolabeled glutaminyl cyclase inhibitor for the potential detection of Alzheimer's disease prior to amyloid β aggregation

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Article information


Submitted
10 Apr 2015
Accepted
21 Apr 2015
First published
22 Apr 2015

Med. Chem. Commun., 2015,6, 1065-1068
Article type
Concise Article

Synthesis and evaluation of [11C]PBD150, a radiolabeled glutaminyl cyclase inhibitor for the potential detection of Alzheimer's disease prior to amyloid β aggregation

A. F. Brooks, I. M. Jackson, X. Shao, G. W. Kropog, P. Sherman, C. A. Quesada and P. J. H. Scott, Med. Chem. Commun., 2015, 6, 1065
DOI: 10.1039/C5MD00148J

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