Journal
BIOCONJUGATE CHEMISTRY
Volume 20, Issue 1, Pages 95-101Publisher
AMER CHEMICAL SOC
DOI: 10.1021/bc8003292
Keywords
-
Categories
Funding
- New Energy and Industrial Technology Development Organization (NEDO)
Ask authors/readers for more resources
We report a novel series of radioiodinated aurone derivatives as probes for imaging A beta plaques in the brains of patients with Alzheimer's disease (AD) using single photon emission computed tomography (SPECT). In binding experiments in vitro, aurone derivatives showed very good affinity for A beta aggregates (K-i = 1.1 to 3.4 nM). No-carrier-added radioiodinated aurones were successfully prepared through an iododestannylation reaction from the corresponding tributyltin derivatives, In biodistribution experiments using normal mice, aurone derivatives displayed high brain uptake (1.7-4.5% ID/g at 2 min) and rapid clearance from the brain (0.1-0.4% ID/g at 30 min), especially [I-121]15. Furthermore, a specific plaque labeling signal was observed in in vitro autoradiography of postmortem AD brain sections using [I-121]15. [I-121]15 may be a useful SPECT imaging agent for detecting A beta plaques in the brain of AD.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available