Rhenium and technetium complexes that bind to amyloid-β plaques

被引：20

作者：

Hayne, David J. ^{[1
,2
]}

North, Andrea J. ^{[1
,2
]}

Fodero-Tavoletti, Michelle ^{[3
,5
]}

White, Jonathan M. ^{[1
,2
]}

Hung, Lin W. ^{[2
,3
]}

Rigopoulos, Angela ^{[4
]}

McLean, Catriona A. ^{[3
,6
]}

Adlard, Paul A. ^{[3
]}

Ackermann, Uwe ^{[5
]}

Tochon-Danguy, Henri ^{[5
]}

Villemagne, Victor L. ^{[3
,5
]}

Barnham, Kevin J. ^{[2
,3
,7
]}

Donnelly, Paul S. ^{[1
,2
]}

机构：

[1] Univ Melbourne, Sch Chem, Melbourne, Vic 3010, Australia

[2] Univ Melbourne, Mol Sci & Biotechnol Inst Bio21, Melbourne, Vic 3010, Australia

[3] Univ Melbourne, Florey Inst Neurosci & Mental Hlth, Melbourne, Vic 3010, Australia

[4] Ludwig Inst Canc Res, Heidelberg, Vic, Australia

[5] Austin Hlth, Dept Mol Imaging & Therapy, Heidelberg, Vic 3084, Australia

[6] Alfred Hosp, Dept Anat Pathol, Prahran, Vic 3181, Australia

[7] Univ Melbourne, Dept Pharmacol, Heidelberg, Vic 3084, Australia

来源：

DALTON TRANSACTIONS | 2015年 / 44卷 / 11期

基金：

澳大利亚研究理事会;

关键词：

PET IMAGING AGENTS; TRICARBONYL COMPLEXES; ALZHEIMERS-DISEASE; P-GLYCOPROTEIN; CRYSTAL; PROBES; STILBENES; STYRYLPYRIDINES; BIOMOLECULES; LIGANDS;

D O I：

10.1039/c4dt02969k

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Alzheimer's disease is associated with the presence of insoluble protein deposits in the brain called amyloid plaques. The major constituent of these deposits is aggregated amyloid-beta peptide. Technetium-99m complexes that bind to amyloid-beta plaques could provide important diagnostic information on amyloid-beta plaque burden using Single Photon Emission Computed Tomography (SPECT). Tridentate ligands with a stilbene functional group were used to form complexes with the fac-[M-I(CO)(3)](+) (M = Re or Tc-99m) core. The rhenium carbonyl complexes with tridentate co-ligands that included a stilbene functional group and a dimethylamino substituent bound to amyloid-beta present in human frontal cortex brain tissue from subjects with Alzheimer's disease. This chemistry was extended to make the analogous [Tc-99m(I)(CO)(3)](+) complexes and the complexes were sufficiently stable in human serum. Whilst the lipophilicity (log D7.4) of the technetium complexes appeared ideally suited for penetration of the blood-brain barrier, preliminary biodistribution studies in an AD mouse model (APP/PS1) revealed relatively low brain uptake (0.24% ID g(-1) at 2 min post injection).

引用

页码：4933 / 4944

页数：12

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