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

Christos Kiritsis, Barbara Mavroidi, Antonio Shegani, Lazaros Palamaris, George Loudos, Marina Sagnou, Ioannis Pirmettis, Minas Papadopoulos, Maria Pelecanou*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1089-1092
Number of pages4
JournalAcs Medicinal Chemistry Letters
Volume8
Issue number10
DOIs
Publication statusPublished - 12 Oct 2017

Keywords

  • Tc
  • 2-(4′-Aminophenyl)benzothiazole
  • cyclopentadienyl
  • Re
  • SPECT imaging
  • β-amyloid plaques

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