Source:http://linkedlifedata.com/resource/pubmed/id/17845017
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
20
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pubmed:dateCreated |
2007-9-27
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pubmed:abstractText |
beta-Amyloid (Abeta) binding affinities and specificities for six bis-styrylbenzenes with multiple magnetically equivalent fluorine atoms in the form of a tetrafluorophenyl core or symmetrical trifluoromethyl and trifluoromethoxy groups were determined by means of fluorescence titrations with amyloid peptide Abeta1-40 and a novel in vitro fluorescence-based assay using APP/PS1 transgenic mouse brain sections. Bis-styrylbenzenes with a tetrafluorophenyl core had increased Abeta binding affinities compared to their monofluorophenyl or phenyl counterparts. Bis-styrylbenzenes with carboxylic acid functional groups had lower Abeta binding affinities than their neutral counterparts. Selected bis-styrylbenzenes were demonstrated to have good blood-brain barrier penetration capabilities. These data extend the SAR of bis-styrylbenzene Abeta binding and provide direction for the development of a noninvasive probe for early detection of Alzheimer's disease using 19F MRI.
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pubmed:grant | |
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/Fluorobenzenes,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Styrenes,
http://linkedlifedata.com/resource/pubmed/chemical/amyloid beta-protein (1-40)
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
4
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4986-92
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:17845017-Amyloid beta-Peptides,
pubmed-meshheading:17845017-Animals,
pubmed-meshheading:17845017-Blood-Brain Barrier,
pubmed-meshheading:17845017-Fluorescence,
pubmed-meshheading:17845017-Fluorobenzenes,
pubmed-meshheading:17845017-Ligands,
pubmed-meshheading:17845017-Mice,
pubmed-meshheading:17845017-Mice, Transgenic,
pubmed-meshheading:17845017-Peptide Fragments,
pubmed-meshheading:17845017-Protein Binding,
pubmed-meshheading:17845017-Stereoisomerism,
pubmed-meshheading:17845017-Structure-Activity Relationship,
pubmed-meshheading:17845017-Styrenes
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pubmed:year |
2007
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pubmed:articleTitle |
Polyfluorinated bis-styrylbenzene beta-amyloid plaque binding ligands.
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pubmed:affiliation |
University of Nebraska Medical Center, College of Pharmacy, 986025 Nebraska Medical Center, Omaha, Nebraska 68198, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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