摘要
阿尔茨海默病(AD)是不可逆性痴呆症中最常见的形式.除了评估AD患者记忆能力,正电子发射断层扫描(PET)作为一种灵敏度较高的非侵入性诊断方式,还可以对靶点进行定性或定量的影像诊断,定性及定量评价β淀粉样蛋白(Aβ)、tau蛋白、突触蛋白等相关生物标志物,对AD诊断具有重要意义.硫代黄素-T衍生物[18F]氟替莫尔和苯乙烯吡啶及二苯乙烯衍生物[18F]氟倍他滨、[18F]氟倍他平能与Aβ高度特异性地结合,作为PET显影剂被FDA批准上市.68Ga、64Cu标记的放射性显影剂同样表现出高度的Aβ斑块亲和力.喹啉衍生物[18F]-THK5351和[18F]-PPQ8、吡啶吲哚衍生物[18F]-T807、兰索拉唑衍生物[11C]-NML均可量化tau蛋白错误折叠导致的神经纤维缠结程度.左乙拉西坦结构衍生物[11C]-UCB-J、[18F]-SDM-8可以测量突触密度,3-氟-4-乙炔基苄腈衍生物[18F]-FPEB则通过与代谢型谷氨酸受体第5亚型(mGluR5)的结合用于AD的辅助诊断,酮色林类衍生物[18F]-altanserin则通过作用于5-羟色胺用于研究早期AD的分子变化.
Abstract
Alzheimer's disease(AD)is the most common form of irreversible dementia.In addition to assessing of patients'memory abilities,positron emission tomography(PET),as a non-invasive diagnostic modality with high sensitivity and qualitative or quantitative imaging of the target sites,can qualitatively and quantitatively evaluate β-amyloid(Aβ),tau proteins,synaptic proteins,and other related biomarkers,which is of great significance in the diagnosis of AD.As PET imaging approved by FDA,[18F]-flutemetamol,a derivative of 18F labelled thioflavin-T,and[18F]-florbetaben,[18F]-florbetapir,which are phenylpyridine derivates,have high specificity in their affinity for Aβ plaque binding.Other radionuclides such as 68Ga and 64Cu labeled radiotracers also showed high affinity with Aβ plaques.Quinoline derivatives[18F]-THK5351,[18F]-PPQ8,benzimidazolopyrimidine and pyridine-indole derivatives[18F]-T807,and lansoprazole derivatives[11C]-NML as PET imaging agents,can quantify tau protein tangles.And the structural derivatives of levetiracetam[11C]-UCB-J and[18F]-SDM-8 can measure synaptic density,while the structural derivatives[18F]-FPEB of 3-fluoro-4-acetylidene-benzylnitrile can assist in the diagnosis of AD by binding with mGluR5.The fluorobenzoyl derivative[18F]-altanserin,with ketoserin as its structural parent,acts on 5-hydroxytryptamine to study the molecular changes of early AD.
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