F 标记突触囊泡糖蛋白 2A PET 成像探针 [F]SynVesT-2 的合成与临床前评价
Synthesis and Preclinical Evaluation of an F-Labeled Synaptic Vesicle Glycoprotein 2A PET Imaging Probe: [F]SynVesT-2.
机构信息
PET Center, Department of Radiology and Biomedical Imaging , Yale University , New Haven , Connecticut 06520 , United States.
Department of Nuclear Medicine, Laboratory of Clinical Nuclear Medicine , West China Hospital, Sichuan University , Chengdu , Sichuan 610041 , China.
出版信息
ACS Chem Neurosci. 2020 Feb 19;11(4):592-603. doi: 10.1021/acschemneuro.9b00618. Epub 2020 Feb 4.
Synaptic vesicle glycoprotein 2A (SV2A) is a 12-pass transmembrane glycoprotein ubiquitously expressed in presynaptic vesicles. imaging of SV2A using PET has potential applications in the diagnosis and prognosis of a variety of neuropsychiatric diseases, e.g., Alzheimer's disease, Parkinson's disease, schizophrenia, multiple sclerosis, autism, epilepsy, stroke, traumatic brain injury, post-traumatic stress disorder, depression, etc. Herein, we report the synthesis and evaluation of a new F-labeled SV2A PET imaging probe, [F]SynVesT-2, which possesses fast binding kinetics and high specific binding signals in non-human primate brain.
突触小泡糖蛋白 2A（SV2A）是一种 12 次跨膜糖蛋白，广泛存在于突触小泡中。使用正电子发射断层扫描（PET）对 SV2A 进行成像，在诊断和预测各种神经精神疾病（如阿尔茨海默病、帕金森病、精神分裂症、多发性硬化症、自闭症、癫痫、中风、创伤性脑损伤、创伤后应激障碍、抑郁症等）方面具有潜在的应用。本文报道了一种新型 F 标记的 SV2A PET 成像探针[F]SynVesT-2 的合成与评价，该探针在非人类灵长类动物大脑中具有快速的结合动力学和高特异性结合信号。
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