以Aβ为靶点的阿尔茨海默病PET显像剂的研究进展

阿尔茨海默病(AD)是一种进行性中枢神经退行性疾病,其确诊主要依据死亡后的病理学检查,但对治疗已无意义,只有早期诊断并干预,才能取得较好的治疗效果。正电子发射断层显像(PET)技术的发展,为早期非侵入性诊断AD提供了可能性。β淀粉样蛋白(Aβ)沉积形成的胞外老年斑沉积(SPs)是AD的重要病理学特征之一,以Aβ为靶点的PET显像剂对AD早期诊断具有重要意义,也是该领域的研究热点。本文介绍了有机小分子类Aβ显像剂的研究进展,主要包括刚果红类、氨基萘类、苯并噻唑类、苯并噻唑衍生类、二苯乙烯类、取代二苯乙烯类和其他有机小分子,总结了Aβ显像剂的理想特征并对Aβ显像剂的发展进行了展望。

Research Progress of Aβ Targeting PET Imaging Agents for Alzheimer’s Disease

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder in central nervous system. The diagnosis of AD is mainly based on pathological examination after death, which shows no value to the treatment of AD. If identified and intervened as early as possible at presymptomatic states, the progression of the disease may be delayed. With the progress of positron emission tomography (PET) imaging in clinic, the diagnosis of AD at the early stage with noninvasive techniques become possible. Extracellular senile plaques (SPs), made of accumulations of β-amyloid (Aβ), is one of the most important neuropathological hallmarks of AD. Aβ targeting PET imaging agents are of great significance to early diagnosis of AD, and are one research focus in this field. The research progress of Aβ imaging agents with a small organic molecule is reviewed, which include several kinds: congo red derivatives, aminonaphtyl derivatives, benzothiazole derivatives, benzothiazole-analogues derivatives, stilbene derivatives, substituted-stilbene derivatives and other derivatives. The ideal characteristics of Aβ imaging agents are summarized, and the trend for developing Aβ imaging agents is discussed.