A dual fluorinated and iodinated radiotracer for PET and SPECT imaging of β-amyloid plaques in the brain

被引：32

作者：

Watanabe, Hiroyuki ^{[1
,2
]}

Ono, Masahiro ^{[1
,2
]}

Kimura, Hiroyuki ^{[1
]}

Kagawa, Shinya ^{[3
]}

Nishii, Ryuichi ^{[3
]}

Fuchigami, Takeshi ^{[2
]}

Haratake, Mamoru ^{[2
]}

Nakayama, Morio ^{[2
]}

Saji, Hideo ^{[1
]}

机构：

[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Dept Pathofunct Bioanal, Sakyo Ku, Kyoto 6068501, Japan

[2] Nagasaki Univ, Grad Sch Biomed Sci, Dept Hyg Chem, Nagasaki 8528521, Japan

[3] Shiga Med Ctr, Res Inst, Moriyama, Shiga 5248524, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 21期

关键词：

Alzheimer's disease; beta-Amyloid peptide; PET; SPECT; Dual imaging; ALZHEIMERS-DISEASE; NEUROFIBRILLARY TANGLES; PROBES; AGENTS; BIODISTRIBUTION; DERIVATIVES; RADIOLIGAND; DOSIMETRY; AURONES;

D O I：

10.1016/j.bmcl.2011.08.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report a fluorinated and iodinated radiotracer as a probe for PET/SPECT to detect of beta-amyloid (A beta) plaques in the brain of patients with Alzheimer's disease (AD). We successfully designed and synthesized the fluorinated and iodinated aurone derivative (3) and its radiolabels ([(125)I]3 and [(18)F]3). In binding experiments in vitro, 3 showed high affinity for A beta aggregates (K(i) = 6.81 nM). In brain sections of AD model mice, 3 intensely stained A beta plaques. Furthermore, a specific plaque labeling signal was observed on the autoradiography of postmortem AD brain sections using [(125)I]3. In biodistribution experiments using normal mice, [(125)I]3 and [(18)F]3 displayed good uptake into and a rapid washout from the brain, properties highly desirable for A beta imaging agents. These results suggest that 3 may function as a PET/SPECT dual imaging agent for detecting A beta plaques in AD brains. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：6519 / 6522

页数：4

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