Oct 24, 2017

2-(4'-Aminophenyl)benzothiazole Labeled with 99m Tc-Cyclopentadienyl for Imaging β-Amyloid Plaques

ACS Medicinal Chemistry Letters
Christos KiritsisMaria Pelecanou

Abstract

The development of a 99mTc-radiotracer for imaging of β-amyloid (Aβ) plaques with single photon emission computed tomography (SPECT) is strongly anticipated to provide a low cost and broadly accessible diagnostic tool for Alzheimer's disease (AD). Within this framework, 2-(4'-aminophenyl)benzothiazole, known to display affinity and specificity for Aβ plaques, has been joined to the tricarbonyl fac-[M(CO)3]+ (M = Re(I), 99mTc(I)) core through the cyclopentadienyl moiety to yield stable, neutral, and lipophilic complexes (Re-1 and 99m Tc-1, respectively). The Re-1 complex was completely characterized with spectroscopic methods and was shown to selectively stain Aβ plaques on sections of human AD brain tissue. The 99m Tc-1 complex displayed satisfactory initial brain uptake (0.53% ID/g at 2 min) and in vivo stability in healthy mice, while in transgenic 5xFAD mice, models for AD, a notable retention in the brain was noted (1.94% ID/g at 90 min). The results are encouraging and contribute to the effort of developing a SPECT amyloid imaging agent.

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Mentioned in this Paper

In Vivo
Brain Diseases
Laboratory Procedures
Human neutrophil peptide 3
Benzothiazole [EPC]
C8orf4 gene
Tomography, Emission-Computed, Single-Photon
APP protein, human
Complex (molecular entity)
Brain

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