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

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, 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.

journal_name

Medchemcomm

journal_title

MedChemComm

authors

Brooks AF,Jackson IM,Shao X,Kropog GW,Sherman P,Quesada CA,Scott PJ

doi

10.1039/C5MD00148J

subject

Has Abstract

pub_date

2015-06-01 00:00:00

pages

1065-1068

issue

6

eissn

2040-2503

issn

2040-2511

journal_volume

6

pub_type

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