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Yousefi BH, Drzezga A, von Reutern B, et al. A Novel (18)F-Labeled Imidazo[2,1-b]benzothiazole (IBT) for High-Contrast PET Imaging of β-Amyloid Plaques. ACS Med Chem Lett. 2011;2(9):673-7doi: 10.1021/ml200123w.
Yousefi, B. H., Drzezga, A., von Reutern, B., Manook, A., Schwaiger, M., Wester, H. J., & Henriksen, G. (2011). A Novel (18)F-Labeled Imidazo[2,1-b]benzothiazole (IBT) for High-Contrast PET Imaging of β-Amyloid Plaques. ACS medicinal chemistry letters, 2(9), 673-7. https://doi.org/10.1021/ml200123w
Yousefi, Behrooz H, et al. "A Novel (18)F-Labeled Imidazo[2,1-b]benzothiazole (IBT) for High-Contrast PET Imaging of β-Amyloid Plaques." ACS medicinal chemistry letters vol. 2,9 (2011): 673-7. doi: https://doi.org/10.1021/ml200123w
Yousefi BH, Drzezga A, von Reutern B, Manook A, Schwaiger M, Wester HJ, Henriksen G. A Novel (18)F-Labeled Imidazo[2,1-b]benzothiazole (IBT) for High-Contrast PET Imaging of β-Amyloid Plaques. ACS Med Chem Lett. 2011 Jul 19;2(9):673-7. doi: 10.1021/ml200123w. eCollection 2011 Sep 08. PMID: 24900362; PMCID: PMC4018122.
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ACS Med Chem Lett. 2011 Jul 19;2(9):673-7. doi: 10.1021/ml200123w. eCollection 2011 Sep 08.

A Novel (18)F-Labeled Imidazo[2,1-b]benzothiazole (IBT) for High-Contrast PET Imaging of β-Amyloid Plaques.

ACS medicinal chemistry letters

Behrooz H Yousefi, Alexander Drzezga, Boris von Reutern, André Manook, Markus Schwaiger, Hans-Jürgen Wester, Gjermund Henriksen

Affiliations

  1. Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München , Ismaninger Strasse 22, 81675 München, Germany.
  2. Lehrstuhl für Pharmazeutische Radiochemie , Walther-Meissner-Strasse 3, 85748 Garching, Germany.

PMID: 24900362 PMCID: PMC4018122 DOI: 10.1021/ml200123w

Abstract

(18)F-labeled imidazo[2,1-b]benzothiazole ([(18)F]8) was synthesized and evaluated as a tracer for cerebral β-amyloid deposits (Aβ) by means of positron emission tomography (PET). [(18)F]8 exhibits a high affinity to Aβ and suitable brain uptake kinetics combined with a high metabolic stability in the brain. In a double transgenic APP/PS1 mouse model of Alzheimer's disease, we demonstrated a specific uptake of [(18)F]8 in Aβ-containing telencephalic brain regions. The specific binding of [(18)F]8 to Aβ was confirmed by regional brain biodistribution and autoradiography and correlated to immunohistochemistry staining. Analysis of brain sections of APP/PS1 mouse injected with a cocktail of [(18)F]8 and reference compound [(3)H]PiB revealed that the two tracers bind to Aβ plaques in the brain of mouse in a comparable binding pattern. [(18)F]8 represents the first high-contrast PET imaging agent for detection of Aβ plaques in transgenic mouse model of Alzheimer's disease and holds promise for transfer to a clinical evaluation.

Keywords: 18F-labeled tracer for β-amyloid; APP/PS1transgenic mice; Alzheimer's disease; IBT; autoradiography; neuroimaging; positron emission tomography; β-amyloid plaques

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