Source:http://linkedlifedata.com/resource/pubmed/id/20089413
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
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| pubmed:dateCreated |
2010-3-15
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| pubmed:abstractText |
Amyloid aggregates play a major role in the development of Alzheimer's disease. Targeting these aggregates by PET probes enables non-invasively the detection and quantification of amyloid deposit distribution in human brains. Based on benzothiazole core structure a series of amyloid imaging agents were developed. Currently [(11)C]2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole (Pittsburgh Compound-B (PIB) is the most specific and widely used amyloid imaging ligand. But due to the short half life of (11)C, longer lived (18)F-labeled derivatives offer logistic advantages and higher contrast images. In this work, three different [(18)F]fluoroethoxy-substituted benzothiazole derivatives ([(18)F]2-(4'-(methylamino)phenyl)-6-(2-fluoroethoxy)benzothiazole, [(18)F]2-((2'-(2-fluoroethoxy)-4'-amino)phenyl)benzothiazole and [(18)F]2-(3'-((2-fluoroethoxy)-4'-amino)phenyl)benzothiazole) were synthesized via [(18)F]fluoroethylation. The latter two derivatives with fluoroethoxy-substitution on the aromatic amino group showed very low binding affinity for amyloid aggregates. In contrast [(18)F]2-(4'-(methylamino)phenyl)-6-(2-fluoroethoxy)benzothiazole with [(18)F]fluoroethoxy-substitution in 6-position showed excellent amyloid imaging properties with respect to lipophilicity, brain entry and brain clearance in normal SCID mice, amyloid plaque binding affinity and specificity.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
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| pubmed:month |
Jun
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| pubmed:issn |
1872-9800
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| pubmed:author | |
| pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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| pubmed:issnType |
Electronic
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| pubmed:volume |
68
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
1066-72
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| pubmed:dateRevised |
2010-11-18
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| pubmed:meshHeading |
pubmed-meshheading:20089413-Alzheimer Disease,
pubmed-meshheading:20089413-Amyloid,
pubmed-meshheading:20089413-Animals,
pubmed-meshheading:20089413-Benzothiazoles,
pubmed-meshheading:20089413-Brain,
pubmed-meshheading:20089413-Fluorine Radioisotopes,
pubmed-meshheading:20089413-Mice,
pubmed-meshheading:20089413-Mice, SCID,
pubmed-meshheading:20089413-Plaque, Amyloid,
pubmed-meshheading:20089413-Positron-Emission Tomography,
pubmed-meshheading:20089413-Radiopharmaceuticals
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| pubmed:year |
2010
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| pubmed:articleTitle |
Synthesis and evaluation of 18F-fluoroethylated benzothiazole derivatives for in vivo imaging of amyloid plaques in Alzheimer's disease.
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| pubmed:affiliation |
Department of Nuclear Medicine, University of Ulm, Ulm, Germany. bernd.neumaier@nf.mpg.de
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| pubmed:publicationType |
Journal Article
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