| 11C-labeled stilbene derivatives as Abeta-aggregate-specific PET imaging agents for Alzheimer's disease. | |
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MedLine Citation:
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PMID: 12900282 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of stilbene derivatives as potential diagnostic imaging agents targeting amyloid plaques in Alzheimer's disease (AD) were synthesized and evaluated. The syntheses of the stilbenes were successfully achieved by a simple Wadsworth-Emmons reaction between diethyl (4-nitrobenzyl)phosphonate and 4-methoxybenzaldehyde. 4-N,N-dimethylamino-4'-methyoxy and the corresponding 4-N-monomethylamino-, 4'-hydroxy stilbenes showed good binding affinities towards Abeta aggregates in vitro (K(i) < 10 nM). The (11)C labeled 4-N-methylamino-4'-hydroxystilbene, [(11)C]4, was prepared by (11)C methylation of 4-amino-4'-hydroxystilbene. The [(11)C]4 displayed a moderate lipophilicity (log P = 2.36), and showed a very good brain penetration and washout from normal rat brain after an iv injection. In vitro autoradiography of transgenic AD mouse brain sections showed a high specific labeling of beta-amyloid plaques, whereas the control sections showed no binding. Taken together the data suggest that a relatively simple stilbene derivative, [(11)C]4, N-[(11)C]methylamino-4'-hydroxystilbene, may be useful as a positron emission tomography (PET) imaging agent for mapping Abeta plaques in the brain of patients with Alzheimer's disease. |
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Authors:
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Masahiro Ono; Alan Wilson; Jose Nobrega; David Westaway; Paul Verhoeff; Zhi-Ping Zhuang; Mei-Ping Kung; Hank F Kung |
Publication Detail:
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Type: Evaluation Studies; Journal Article |
Journal Detail:
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Title: Nuclear medicine and biology Volume: 30 ISSN: 0969-8051 ISO Abbreviation: Nucl. Med. Biol. Publication Date: 2003 Aug |
Date Detail:
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Created Date: 2003-08-05 Completed Date: 2004-05-17 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9304420 Medline TA: Nucl Med Biol Country: England |
Other Details:
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Languages: eng Pagination: 565-71 Citation Subset: IM |
Affiliation:
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Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Alzheimer Disease
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diagnosis*,
metabolism* Amyloid beta-Protein / metabolism* Animals Autoradiography Brain / metabolism*, radionuclide imaging* Carbon Radioisotopes / chemistry, diagnostic use, pharmacokinetics Isotope Labeling / methods Male Mice Mice, Transgenic Radiopharmaceuticals / chemical synthesis, diagnostic use, pharmacokinetics Rats Rats, Sprague-Dawley Stilbenes / diagnostic use*, pharmacokinetics* Tissue Distribution Tomography, Emission-Computed / methods* |
| Chemical | |
Reg. No./Substance:
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0/Amyloid beta-Protein; 0/Carbon Radioisotopes; 0/Radiopharmaceuticals; 0/Stilbenes |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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