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Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.设计和选择参数以加速新型中枢神经系统正电子发射断层扫描(PET)配体的发现及其在新型磷酸二酯酶 2A PET 配体开发中的应用。
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用于神经退行性疾病的正电子发射断层显像/单光子发射计算机断层显像成像剂。

PET/SPECT imaging agents for neurodegenerative diseases.

作者信息

Zhu Lin, Ploessl Karl, Kung Hank F

机构信息

Beijing Institute for Brain Disorders, Capital Medical University, Beijing, China.

出版信息

Chem Soc Rev. 2014 Oct 7;43(19):6683-91. doi: 10.1039/c3cs60430f.

DOI:10.1039/c3cs60430f
PMID:24676152
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4159420/
Abstract

Single photon emission computed tomography (SPECT) or positron emission computed tomography (PET) imaging agents for neurodegenerative diseases have a significant impact on clinical diagnosis and patient care. The examples of Parkinson's Disease (PD) and Alzheimer's Disease (AD) imaging agents described in this paper provide a general view on how imaging agents, i.e. radioactive drugs, are selected, chemically prepared and applied in humans. Imaging the living human brain can provide unique information on the pathology and progression of neurodegenerative diseases, such as AD and PD. The imaging method will also facilitate preclinical and clinical trials of new drugs offering specific information related to drug binding sites in the brain. In the future, chemists will continue to play important roles in identifying specific targets, synthesizing target-specific probes for screening and ultimately testing them by in vitro and in vivo assays.

摘要

用于神经退行性疾病的单光子发射计算机断层扫描(SPECT)或正电子发射计算机断层扫描(PET)成像剂对临床诊断和患者护理具有重大影响。本文所述的帕金森病(PD)和阿尔茨海默病(AD)成像剂的例子,提供了关于成像剂(即放射性药物)如何被选择、化学制备以及应用于人体的总体情况。对活体人类大脑进行成像可以提供有关神经退行性疾病(如AD和PD)的病理学和进展的独特信息。成像方法还将促进新药的临床前和临床试验,提供与大脑中药物结合位点相关的特定信息。未来,化学家将继续在识别特定靶点、合成用于筛选的靶点特异性探针并最终通过体外和体内试验对其进行测试方面发挥重要作用。