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001     136683
005     20250717152604.0
024 7 _ |a 10.1021/jm300653b
|2 doi
024 7 _ |a pmid:22913544
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024 7 _ |a 0022-2623
|2 ISSN
024 7 _ |a 0095-9065
|2 ISSN
024 7 _ |a 1520-4804
|2 ISSN
024 7 _ |a 1943-2992
|2 ISSN
024 7 _ |a altmetric:35469014
|2 altmetric
037 _ _ |a DZNE-2020-03005
041 _ _ |a English
082 _ _ |a 610
100 1 _ |a Boländer, Alexander
|0 P:(DE-HGF)0
|b 0
245 _ _ |a Bis(arylvinyl)pyrazines, -pyrimidines, and -pyridazines as imaging agents for tau fibrils and β-amyloid plaques in Alzheimer's disease models.
260 _ _ |a Washington, DC
|c 2012
|b ACS
264 _ 1 |3 online
|2 Crossref
|b American Chemical Society (ACS)
|c 2012-08-31
264 _ 1 |3 print
|2 Crossref
|b American Chemical Society (ACS)
|c 2012-11-08
336 7 _ |a article
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336 7 _ |a Output Types/Journal article
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336 7 _ |a Journal Article
|b journal
|m journal
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|s 1752758723_27527
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336 7 _ |a ARTICLE
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336 7 _ |a JOURNAL_ARTICLE
|2 ORCID
336 7 _ |a Journal Article
|0 0
|2 EndNote
520 _ _ |a The in vivo diagnosis of Alzheimer's disease (AD) is of high socioeconomic interest and remains a demanding field of research. The biopathological hallmarks of the disease are extracellular plaques consisting of aggregated β-amyloid peptides (Aβ) and tau protein derived intracellular tangles. Here we report the synthesis and evaluation of fluorescent pyrazine, pyrimidine,and pyridazine derivatives in vitro and in vivo aiming at a tau-based diagnosis of AD. The probes were pre-evaluated on human brain tissue by fluorescence microscopy and were found to label all known disease-related alterations at high contrast and specificity. To quantify the binding affinity, a new thiazine red displacement assay was developed and selected candidates were toxicologically profiled. The application in transgenic mouse models demonstrated bioavailability and brain permeability for one compound. In the course of histological testing, we discovered an AD-related deposition of tau aggregates in the Bowman's glands of the olfactory epithelium, which holds potential for an endoscopic diagnosis of AD in the olfactory system.
536 _ _ |a 342 - Disease Mechanisms and Model Systems (POF3-342)
|0 G:(DE-HGF)POF3-342
|c POF3-342
|f POF III
|x 0
588 _ _ |a Dataset connected to CrossRef, PubMed,
650 _ 7 |a Fluorescent Dyes
|2 NLM Chemicals
650 _ 7 |a Pyrazines
|2 NLM Chemicals
650 _ 7 |a Pyridazines
|2 NLM Chemicals
650 _ 7 |a Pyrimidines
|2 NLM Chemicals
650 _ 7 |a tau Proteins
|2 NLM Chemicals
650 _ 2 |a Aged, 80 and over
|2 MeSH
650 _ 2 |a Alzheimer Disease: diagnosis
|2 MeSH
650 _ 2 |a Alzheimer Disease: metabolism
|2 MeSH
650 _ 2 |a Animals
|2 MeSH
650 _ 2 |a Biological Availability
|2 MeSH
650 _ 2 |a Brain: metabolism
|2 MeSH
650 _ 2 |a Fluorescent Dyes: chemical synthesis
|2 MeSH
650 _ 2 |a Fluorescent Dyes: chemistry
|2 MeSH
650 _ 2 |a Fluorescent Dyes: pharmacokinetics
|2 MeSH
650 _ 2 |a Humans
|2 MeSH
650 _ 2 |a Mice
|2 MeSH
650 _ 2 |a Mice, Transgenic
|2 MeSH
650 _ 2 |a Microscopy, Fluorescence
|2 MeSH
650 _ 2 |a Olfactory Mucosa: metabolism
|2 MeSH
650 _ 2 |a Organ Specificity
|2 MeSH
650 _ 2 |a Permeability
|2 MeSH
650 _ 2 |a Plaque, Amyloid: metabolism
|2 MeSH
650 _ 2 |a Pyrazines: chemical synthesis
|2 MeSH
650 _ 2 |a Pyrazines: chemistry
|2 MeSH
650 _ 2 |a Pyrazines: pharmacokinetics
|2 MeSH
650 _ 2 |a Pyridazines: chemical synthesis
|2 MeSH
650 _ 2 |a Pyridazines: chemistry
|2 MeSH
650 _ 2 |a Pyridazines: pharmacokinetics
|2 MeSH
650 _ 2 |a Pyrimidines: chemical synthesis
|2 MeSH
650 _ 2 |a Pyrimidines: chemistry
|2 MeSH
650 _ 2 |a Pyrimidines: pharmacokinetics
|2 MeSH
650 _ 2 |a Stereoisomerism
|2 MeSH
650 _ 2 |a Structure-Activity Relationship
|2 MeSH
650 _ 2 |a tau Proteins: metabolism
|2 MeSH
700 1 _ |a Kieser, Daniel
|0 P:(DE-HGF)0
|b 1
700 1 _ |a Voss, Constantin
|0 P:(DE-HGF)0
|b 2
700 1 _ |a Bauer, Silvia
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700 1 _ |a Schön, Christian
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700 1 _ |a Burgold, Steffen
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700 1 _ |a Bittner, Tobias
|0 P:(DE-2719)9000029
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700 1 _ |a Hölzer, Jana
|0 P:(DE-HGF)0
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700 1 _ |a Heyny-von Haußen, Roland
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700 1 _ |a Mall, Gerhard
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700 1 _ |a Goetschy, Valérie
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700 1 _ |a Czech, Christian
|0 P:(DE-HGF)0
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700 1 _ |a Knust, Henner
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700 1 _ |a Berger, Robert
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700 1 _ |a Herms, Jochen
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700 1 _ |a Hilger, Ingrid
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700 1 _ |a Schmidt, Boris
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|e Corresponding author
773 1 8 |a 10.1021/jm300653b
|b : American Chemical Society (ACS), 2012-08-31
|n 21
|p 9170-9180
|3 journal-article
|2 Crossref
|t Journal of Medicinal Chemistry
|v 55
|y 2012
|x 0022-2623
773 _ _ |a 10.1021/jm300653b
|g Vol. 55, no. 21, p. 9170 - 9180
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|t Journal of medicinal chemistry
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|y 2012
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856 4 _ |u https://pub.dzne.de/record/136683/files/DZNE-2020-03005_Restricted.pdf
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910 1 _ |a Deutsches Zentrum für Neurodegenerative Erkrankungen
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LibraryCollectionCLSMajorCLSMinorLanguageAuthor
Marc 21