Characterization of a Brain Permeant Fluorescent Molecule and Visualization of Aβ Parenchymal Plaques, Using Real-Time Multiphoton Imaging in Transgenic Mice

Characterization of a Brain Permeant Fluorescent Molecule and Visualization of Aβ Parenchymal Plaques, Using Real-Time Multiphoton Imaging in Transgenic Mice

Emerging paradigms mandate discovery of imaging agents for diagnosing Alzheimer’s disease (AD) prior to appearance of clinical symptoms. To accomplish this objective, a novel heterocyclic molecule (4) was synthesized and validated as Aβ targeted probe. The agent shows labeling of numerous diffuse Aβ...

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Veröffentlicht in:Organic letters 2014-07, Vol.16 (14), p.3640-3643
Hauptverfasser: Sundaram, G.S.M, Garai, Kanchan, Rath, Nigam P, Yan, Ping, Cirrito, John R, Cairns, Nigel J, Lee, Jin-Moo, Sharma, Vijay
Format: Artikel
Sprache:eng
Schlagworte:
Alzheimer Disease - pathology
Animals
Benzothiazoles - chemical synthesis
Benzothiazoles - chemistry
Brain - pathology
Coloring Agents
Diagnostic Imaging
Fluorescent Dyes - chemical synthesis
Fluorescent Dyes - chemistry
Humans
Letter
Male
Mice
Mice, Transgenic
Molecular Structure
Plaque, Amyloid - pathology
Positron-Emission Tomography
Pyridines - chemical synthesis
Pyridines - chemistry
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Zusammenfassung:Emerging paradigms mandate discovery of imaging agents for diagnosing Alzheimer’s disease (AD) prior to appearance of clinical symptoms. To accomplish this objective, a novel heterocyclic molecule (4) was synthesized and validated as Aβ targeted probe. The agent shows labeling of numerous diffuse Aβ plaques in confirmed AD human brain tissues and traverses the blood–brain barrier to enable labeling of parenchymal Aβ plaques in live mice (APP±/PS1±) brains.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol501264q