Chemistry Department, Lomonosov Moscow State University, Leninskie Gory 1,3, 119991 Moscow, Russia.
Department of Materials Science of Semiconductors and Dielectrics, National University of Science and Technology (MISIS), Leninskiy Prospect 4, 101000 Moscow, Russia.
Int J Mol Sci. 2020 Dec 2;21(23):9190. doi: 10.3390/ijms21239190.
One of the hallmarks of Alzheimer's disease (AD) is the deposition of amyloid plaques in the brain parenchyma, which occurs 7-15 years before the onset of cognitive symptoms of the pathology. Timely diagnostics of amyloid formations allows identifying AD at an early stage and initiating inhibitor therapy, delaying the progression of the disease. However, clinically used radiopharmaceuticals based on C and F are synchrotron-dependent and short-lived. The design of new metal-containing radiopharmaceuticals for AD visualization is of interest. The development of coordination compounds capable of effectively crossing the blood-brain barrier (BBB) requires careful selection of a ligand moiety, a metal chelating scaffold, and a metal cation, defining the method of supposed Aβ visualization. In this review, we have summarized metal-containing drugs for positron emission tomography (PET), magnetic resonance imaging (MRI), and single-photon emission computed tomography (SPECT) imaging of Alzheimer's disease. The obtained data allow assessing the structure-ability to cross the BBB ratio.
阿尔茨海默病(AD)的标志之一是淀粉样斑块在脑实质中的沉积,这发生在认知症状出现前 7-15 年。淀粉样蛋白形成的及时诊断可以在早期识别 AD 并启动抑制剂治疗,从而延缓疾病的进展。然而,临床上使用的基于 C 和 F 的放射性药物是依赖同步加速器的且寿命短。因此,设计用于 AD 可视化的新型含金属放射性药物具有重要意义。为了使配位化合物能够有效地穿过血脑屏障(BBB),需要仔细选择配体部分、金属螯合支架和金属阳离子,从而确定假定的 Aβ可视化方法。在这篇综述中,我们总结了用于正电子发射断层扫描(PET)、磁共振成像(MRI)和单光子发射计算机断层扫描(SPECT)成像的含金属药物,以评估其结构-能够穿过 BBB 的比值。