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rdf:type |
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lifeskim:mentions |
umls-concept:C0009742,
umls-concept:C0011923,
umls-concept:C0025936,
umls-concept:C0026018,
umls-concept:C0332461,
umls-concept:C0962722,
umls-concept:C1143503,
umls-concept:C1521801,
umls-concept:C1527240,
umls-concept:C1723136,
umls-concept:C1869507,
umls-concept:C2354310
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pubmed:issue |
9
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pubmed:dateCreated |
2002-9-16
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pubmed:abstractText |
The identification of amyloid deposits in living Alzheimer disease (AD) patients is important for both early diagnosis and for monitoring the efficacy of newly developed anti-amyloid therapies. Methoxy-X04 is a derivative of Congo red and Chrysamine-G that contains no acid groups and is therefore smaller and much more lipophilic than Congo red or Chrysamine-G. Methoxy-X04 retains in vitro binding affinity for amyloid beta (Abeta) fibrils (Ki = 26.8 nM) very similar to that of Chrysamine-G (Ki = 25.3 nM). Methoxy-X04 is fluorescent and stains plaques, tangles, and cerebrovascular amyloid in postmortem sections of AD brain with good specificity. Using multiphoton microscopy to obtain high-resolution (1 microm) fluorescent images from the brains of living PSI/APP mice, individual plaques could be distinguished within 30 to 60 min after a single i.v. injection of 5 to 10 mg/kg methoxy-X04. A single i.p. injection of 10 mg/kg methoxy-X04 also produced high contrast images of plaques and cerebrovascular amyloid in PSI/APP mouse brain. Complementary quantitative studies using tracer doses of carbon- 11-labeled methoxy-X04 show that it enters rat brain in amounts that suggest it is a viable candidate as a positron emission tomography (PET) amyloid-imaging agent for in vivo human studies.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0022-3069
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
61
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
797-805
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:12230326-Alkenes,
pubmed-meshheading:12230326-Alzheimer Disease,
pubmed-meshheading:12230326-Amyloid beta-Peptides,
pubmed-meshheading:12230326-Animals,
pubmed-meshheading:12230326-Benzene,
pubmed-meshheading:12230326-Benzene Derivatives,
pubmed-meshheading:12230326-Binding, Competitive,
pubmed-meshheading:12230326-Blood-Brain Barrier,
pubmed-meshheading:12230326-Carbon Radioisotopes,
pubmed-meshheading:12230326-Coloring Agents,
pubmed-meshheading:12230326-Congo Red,
pubmed-meshheading:12230326-Disease Models, Animal,
pubmed-meshheading:12230326-Imaging, Three-Dimensional,
pubmed-meshheading:12230326-Male,
pubmed-meshheading:12230326-Mice,
pubmed-meshheading:12230326-Mice, Transgenic,
pubmed-meshheading:12230326-Microscopy,
pubmed-meshheading:12230326-Peptide Fragments,
pubmed-meshheading:12230326-Plaque, Amyloid,
pubmed-meshheading:12230326-Rats,
pubmed-meshheading:12230326-Rats, Sprague-Dawley,
pubmed-meshheading:12230326-Sensitivity and Specificity
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pubmed:year |
2002
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pubmed:articleTitle |
Imaging Abeta plaques in living transgenic mice with multiphoton microscopy and methoxy-X04, a systemically administered Congo red derivative.
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pubmed:affiliation |
Department of Psychiatry, University of Pittsburgh School of Medicine, Pennsylvania 15213, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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