期刊
BIOCONJUGATE CHEMISTRY
卷 27, 期 10, 页码 2493-2504出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.6b00444
关键词
-
类别
资金
- National Natural Science Foundation of China [21571022, 81571230]
- National Science and Technology Major Projects for Major New Drugs Innovation and Development [2014ZX09507007-002]
- science and technology project of Beijing Municipal Education Commission [KM20131002500231172293]
- Beijing Municipal Administration of Hospitals Incubating Program [PX2016016]
A series of 2-arylbenzothiazole derivatives conjugated with bis(aminoethanethiol) (BAT) chelating groups were designed and synthesized. A competitive binding assay-based screening was used to select seven rhenium complexes with potent binding affinity toward A beta(1-42) aggregates (K-i < 50 nM) for Tc-99m labeling and further evaluation. The Tc-99m-labeled probes showed good affinity and specificity to A beta plaques in Tg mouse brain tissue in in vitro autoradiography studies. Moreover, [Tc-99m]14b exhibited favorable brain pharmacokinetics in normal mice (2.11% ID/g at 2 min and 0.62% ID/g at 60 min). Ex vivo autoradiography revealed extensive labeling of A beta plaques by [Tc-99m]14b in the brain of Tg mice. Furthermore, we performed the first single-photon emission computed tomography (SPECT) imaging study in nonhuman primates with Tc-99m-labeled A beta probes. The semiquantitative data showed that [Tc-99m]14b penetrated the brains of rhesus monkeys. These results indicate that [Tc-99m]14b could be utilized as a SPECT imaging probe for A beta plaques.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据