Bibliographic Details
| Title: |
Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes |
| Authors: |
PENG Cheng, CUI Meng-chao, LIANG Zhi-gang, LIU Ting-ting |
| Source: |
Journal of Isotopes, Vol 28, Iss 4, Pp 253-258 (2015) |
| Publisher Information: |
Editorial Board of Journal of Isotopes, 2015. |
| Publication Year: |
2015 |
| Collection: |
LCC:Nuclear and particle physics. Atomic energy. Radioactivity |
| Subject Terms: |
Alzheimer’s disease, A&beta, plaques, autoradiography, biodistribution, Nuclear and particle physics. Atomic energy. Radioactivity, QC770-798 |
| More Details: |
In continuation of the investigation on the bithiophene structure as potential Aβ probes, two halogenated chalcone derivatives containing bithiophene moiety were designed and evaluated as imaging probes for Aβ plaques. In vitro fluorescence staining indicated that they could stain Aβ plaques in the brain sections of AD model mice specifically, in vitro binding assay further confirmed that they displayed high binding affinities to Aβ aggregates (Ki=2.33 nM and 0.88 nM). One radio-iodinated probe, 125I labeleled chalcone derivatives was obtained via iododestannylation reaction with high radiochemical yield and purity (>99%). Moreover, the 125I-labeling compound displayed specific labeling of Aβ plaques in the brain sections of AD model mice with low background, and the specific labeling could be confirmed by thioflavin-S staining. In vivo biodistribution in normal mice indicated that the 125I labeling compound exhibited low initial brain uptake (1.19%ID/g at 2 min) and rapid clearance. These preliminary results suggest that 125I labeling compound may serve as novel Aβ imaging probe, although further modifications are needed to improve initial brain uptake. |
| Document Type: |
article |
| File Description: |
electronic resource |
| Language: |
Chinese |
| ISSN: |
1000-7512 |
| Relation: |
http://www.tws.org.cn/CN/10.7538/tws.2015.28.04.0253; https://doaj.org/toc/1000-7512 |
| DOI: |
10.7538/tws.2015.28.04.0253 |
| Access URL: |
https://doaj.org/article/e4a4c8f4461d4d22853300266a3dcb75 |
| Accession Number: |
edsdoj.4a4c8f4461d4d22853300266a3dcb75 |
| Database: |
Directory of Open Access Journals |
