Linked Life Data

18550375

Source:http://linkedlifedata.com/resource/pubmed/id/18550375

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
14
pubmed:dateCreated
2008-7-25
pubmed:abstractText
In the search for novel probes for the imaging in vivo of beta-amyloid plaques in Alzheimer's disease (AD) brain, we have synthesized and evaluated a series of 3,5-diphenyl-1,2,4-oxadiazole (DPOD) derivatives. The affinity for beta-amyloid plaques was assessed by an in vitro-binding assay using pre-formed synthetic Abeta42 aggregates. The new series of DPOD derivatives showed excellent affinity for Abeta aggregates with K(i) values ranging from 4 to 47nM. In biodistribution experiments using normal mice, [(125)I]12, [(125)I]13, [(125)I]14, and [(125)I]15 examined displayed sufficient uptake for imaging, ranging from 2.2 to 3.3% ID/g. But the washout of the four ligands from the brain was relatively slow. Although additional modifications are necessary to improve the uptake and rapid clearance of non-specifically bound radiotracers, the DPOD pharmacophore with high-binding affinity for Abeta aggregates may be useful as a backbone structure to develop novel beta-amyloid imaging agents.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
1464-3391
pubmed:author
pubmed:issnType
Electronic
pubmed:day
15
pubmed:volume
16
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
6867-72
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
Development of novel beta-amyloid probes based on 3,5-diphenyl-1,2,4-oxadiazole.
pubmed:affiliation
Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan. ono@pharm.kyoto-u.ac.jp
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't