| 引用本文: | 胡梅,刘楠,陈跃,王力.基于突触囊泡蛋白2A成像的正电子发射断层显像剂的合成及临床研究进展[J].中国现代应用药学,2022,39(3):417-423. |
| HU Mei,LIU Nan,CHEN Yue,WANG Li.Synthesis and Clinical Research Progress of Positron Emission Tomography Imaging Agent Based on Synaptic Vesicle Protein 2A Imaging[J].Chin J Mod Appl Pharm(中国现代应用药学),2022,39(3):417-423. |
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| 基于突触囊泡蛋白2A成像的正电子发射断层显像剂的合成及临床研究进展 |
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胡梅1,2,3,4, 刘楠1,2,3, 陈跃1,2,3, 王力1,2,3
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1.西南医科大学附属医院核医学科, 四川 泸州 646000;2.核医学与分子影像四川省重点实验室, 四川 泸州 646000;3.四川省院士(专家)工作站, 四川 泸州 646000;4.西南医科大学药学院, 四川 泸州 646000
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| 摘要: |
| 神经突触异常与多种神经精神疾病有关，包括癫痫、阿尔茨海默病和精神分裂症等。神经突触囊泡蛋白2A（synaptic vesicle protein 2A，SV2A）在中枢神经系统的神经元中广泛表达，由于靶向SV2A的药物在神经退行性疾病和精神疾病中的潜在价值，研究人员对使用靶向SV2A的正电子发射断层扫描显像剂表现出越来越多的关注。在过去的十年中，已经开发了几种SV2A的正电子发射断层显像剂，以实现体内突触的可视化和定量。研究人员使用C-11或F-18对药物进行放射性标记，然后注入啮齿动物和非人类灵长类动物体内进行临床前研究，应用不同的动力学建模方法对药物进入体内效果进行定量分析。本文综述了这些正电子发射断层扫描显像剂的放射合成方法，并通过聚焦其放射化学特性介绍它们的前景和局限性，以及临床前概念验证和目前进行的主要临床研究。 |
| 关键词: 突触囊泡蛋白2A PET放射性示踪剂 突触丧失 放射化学 临床研究 |
| DOI：10.13748/j.cnki.issn1007-7693.2022.03.023 |
| 分类号:R914.5;R969.4 |
| 基金项目:核医学与分子影像四川省重点实验室课题（HYX18005） |
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| Synthesis and Clinical Research Progress of Positron Emission Tomography Imaging Agent Based on Synaptic Vesicle Protein 2A Imaging |
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HU Mei1,2,3,4, LIU Nan1,2,3, CHEN Yue1,2,3, WANG Li1,2,3
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1.Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou 646000, China;2.Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou 646000, China;3.Academician(Expert) Workstation of Sichuan Province, Luzhou 646000, China;4.School of Pharmacy, Southwest Medical University, Luzhou 646000, China
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| Abstract: |
| Synaptic abnormalities are related to a variety of neuropsychiatric diseases, including epilepsy, Alzheimer's disease and schizophrenia. Synaptic vesicle protein 2A(SV2A) is widely expressed in neurons of the central nervous system. Due to the potential value of drugs targeting SV2A in neurodegenerative diseases and mental diseases, researchers have shown increasing concern about the use of positron emission tomography imaging agents targeting SV2A. In the past decade, several positron emission tomography imaging agents of SV2A protein have been developed to realize the visualization and quantification of synapses in vivo. Researchers use C-11 or F-18 to radioactively label the drug, and then inject it into rodents and non-human primates for preclinical studies, and apply different kinetic modeling methods to quantitatively analyze the effects of drugs entering the body. This review describes the radiation synthesis methods of these positron emission tomography imaging agents, and introduces their limitations and prospects by focusing on their radiochemistry properties, as well as preclinical proof of concept and major clinical studies currently in progress. |
| Key words: synaptic vesicle protein 2A PET radiotracer synapse loss radiochemistry clinical research |
