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ACS Med Chem Lett. 2017 Sep 18;8(10):1089-1092. doi: 10.1021/acsmedchemlett.7b00294. eCollection 2017.

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

Author information

  • 1Institutes of Nuclear & Radiological Sciences & Technology, Energy & Safety and Biosciences & Applications, National Centre for Scientific Research "Demokritos", 15310 Athens, Greece.
  • 2Department of Medical Instruments Technology, Technological Educational Institute, 12210 Athens, Greece.

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 99mTc-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 99mTc-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.

KEYWORDS:

2-(4′-Aminophenyl)benzothiazole; 99mTc; Re; SPECT imaging; cyclopentadienyl; β-amyloid plaques

PMID:
29057056
PMCID:
PMC5641965
[Available on 2018-10-12]
DOI:
10.1021/acsmedchemlett.7b00294
[PubMed]
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