当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Novel (E)-5-styryl-2,2'-bithiophene derivatives as ligands for β-amyloid plaques.

Novel (E)-5-styryl-2,2'-bithiophene derivatives as ligands for β-amyloid plaques.

Abstract：

:In continuation of our investigation on the bithiophene structure as potential β-amyloid probes, a series of (E)-5-styryl-2,2'-bithiophene (SBTP) derivatives was designed and synthesized. In vitro binding showed that all of them displayed high binding affinities to Aβ(1-42) aggregates (K(i)=0.10-41.05nM). Moreover, two radio-iodinated probes, [(125)I]-(E)-5-(4-iodostyryl)-2,2'-bithiophene ([(125)I]8) and [(125)I]-(E)-5-iodo-5'-(4-methoxystyryl)-2,2'-bithiophene ([(125)I]31) were prepared. Both of them displayed specific labeling of Aβ plaques in the brain sections of AD model mice with low background. In vivo biodistribution in normal mice indicated that [(125)I]8 exhibited high initial brain uptake (2.11% ID/g at 2 min) and rapid clearance (0.41% ID/g at 30 min). These preliminary results suggest that SBTP derivatives may be served as novel β-amyloid imaging probes.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Cui M,Li Z,Tang R,Jia H,Liu B

doi

10.1016/j.ejmech.2011.04.015

subject

Has Abstract

pub_date

2011-07-01 00:00:00

pages

2908-16

issue

7

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00300-X

journal_volume

46

pub_type

杂志文章

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