Source:http://linkedlifedata.com/resource/pubmed/id/20605471
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
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pubmed:dateCreated |
2011-3-25
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pubmed:abstractText |
We synthesized a novel series of phenylindole (PI) derivatives and evaluated their biological activities as probes for imaging A? plaques in vivo. The affinity for A? plaques was assessed by an in vitro-binding assay using pre-formed synthetic A? aggregates. 2-phenyl-1H-indole (2-PI) derivatives showed high affinity for A?42 aggregates with K(i) values ranging from 4 to 32 nM. 2-PI derivatives clearly stained A? plaques in an animal model of AD. In biodistribution experiments using normal mice, 2-PI derivatives displayed sufficient uptake for imaging, ranging from 1.1% to 2.6% ID/g. Although additional modifications are necessary to improve uptake by and clearance from the brain, 2-PI derivatives may be useful as a backbone structure to develop novel A? imaging agents.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amyloid beta-Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals,
http://linkedlifedata.com/resource/pubmed/chemical/amyloid beta-protein (1-42)
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1464-3391
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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:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4740-6
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pubmed:meshHeading |
pubmed-meshheading:20605471-Amyloid beta-Peptides,
pubmed-meshheading:20605471-Animals,
pubmed-meshheading:20605471-Brain,
pubmed-meshheading:20605471-Indoles,
pubmed-meshheading:20605471-Mice,
pubmed-meshheading:20605471-Peptide Fragments,
pubmed-meshheading:20605471-Plaque, Amyloid,
pubmed-meshheading:20605471-Radiopharmaceuticals,
pubmed-meshheading:20605471-Tissue Distribution,
pubmed-meshheading:20605471-Tomography, Emission-Computed, Single-Photon
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pubmed:year |
2010
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pubmed:articleTitle |
Synthesis and characterization of novel phenylindoles as potential probes for imaging of ?-amyloid plaques in the brain.
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pubmed:affiliation |
Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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