Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
13
pubmed:dateCreated
2011-3-25
pubmed:abstractText
We synthesized a novel series of phenylindole (PI) derivatives and evaluated their biological activities as probes for imaging A? plaques in vivo. The affinity for A? plaques was assessed by an in vitro-binding assay using pre-formed synthetic A? aggregates. 2-phenyl-1H-indole (2-PI) derivatives showed high affinity for A?42 aggregates with K(i) values ranging from 4 to 32 nM. 2-PI derivatives clearly stained A? plaques in an animal model of AD. In biodistribution experiments using normal mice, 2-PI derivatives displayed sufficient uptake for imaging, ranging from 1.1% to 2.6% ID/g. Although additional modifications are necessary to improve uptake by and clearance from the brain, 2-PI derivatives may be useful as a backbone structure to develop novel A? 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:copyrightInfo
Copyright © 2010 Elsevier Ltd. All rights reserved.
pubmed:issnType
Electronic
pubmed:day
1
pubmed:volume
18
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4740-6
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Synthesis and characterization of novel phenylindoles as potential probes for imaging of ?-amyloid plaques in the brain.
pubmed:affiliation
Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't