| Autor: |
Chao, Zheng, Daniel, Holden, Ming-Qiang, Zheng, Richard, Pracitto, Kyle C, Wilcox, Marcel, Lindemann, Zachary, Felchner, Li, Zhang, Jie, Tong, Krista, Fowles, Sjoerd J, Finnema, Nabeel, Nabulsi, Richard E, Carson, Yiyun, Huang, Zhengxin, Cai |
| Rok vydání: |
2021 |
| Předmět: |
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| Zdroj: |
European journal of nuclear medicine and molecular imaging. 49(5) |
| ISSN: |
1619-7089 |
| Popis: |
To quantify the synaptic vesicle glycoprotein 2A (SV2A) changes in the whole central nervous system (CNS) under pathophysiological conditions, a high affinity SV2A PET radiotracer with improved in vivo stability is desirable to minimize the potential confounding effect of radiometabolites. The aim of this study was to develop such a PET tracer based on the molecular scaffold of UCB-A, and evaluate its pharmacokinetics, in vivo stability, specific binding, and nonspecific binding signals in nonhuman primate brains, in comparison with [The racemic SDM-16 (4-(3,5-difluorophenyl)-1-((2-methyl-1H-imidazol-1-yl)methyl)pyrrolidin-2-one) and its two enantiomers were synthesized and assayed for in vitro binding affinities to human SV2A. We synthesized the enantiopure [SDM-16 was synthesized in 3 steps with 44% overall yield and has the highest affinity (KWe have successfully synthesized a novel SV2A PET tracer [ |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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