Development and evaluation of iodinated tracers targeting amyloid plaques for SPECT Imaging
Development and evaluation of iodinated tracers targeting amyloid plaques for SPECT Imaging
复制标题
DOI：
10.1385/jmn:24:1:049
复制
发表时间：
2004-01-01
影响因子：
3.1
通讯作者：
Kung, HF
中科院分区：
文献类型：
--
作者：
Kung, MP;Zhuang, ZP;Kung, HF
各种神经递质受体的碘化配体的成功开发促使我们探索利用碘化配体靶向阿尔茨海默病淀粉样斑块的可行性。为此目的，已经成功制备并评估了几种基于各种化学主链结构的潜在碘化示踪剂。对于这些配体，一致观察到 Abeta 聚集体的高结合亲和力。然而，大多数这些碘化配体通常缺乏所需的体内特性。只有具有良好的体外和体内特性（例如 IMPY）的配体才可能保证其成功成为绘制活人大脑中淀粉样蛋白斑块的潜在显像剂。
Successful development of iodinated ligands for various neurotransmitter receptors prompted us to explore the feasability of having iodinated ligands to target amyloid plaques of Alzheimer's disease. Several potential iodinated tracers based on various chemical backbone structures have been successfully prepared and evaluated toward this purpose. High binding affinities for Abeta aggregates were consistently observed for those ligands. However, the desirable in vivo properties were generally missing in the majority of those iodinated ligands. Only ligands with the promising in vitro and in vivo characteristics such as IMPY will likely warrant their success to be potential imaging agents mapping amyloid plaques in living human brain.