基于（S）-西酞普兰的新型高亲和力血清素转运体荧光配体。
Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.
作者信息
Kumar Vivek, Rahbek-Clemmensen Troels, Billesbølle Christian B, Jorgensen Trine Nygaard, Gether Ulrik, Newman Amy Hauck
机构信息
Medicinal Chemistry Section, Molecular Targets and Medications Discovery Branch, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health , 333 Cassell Drive, Baltimore, Maryland 21224, United States.
Molecular Neuropharmacology Laboratory and Center for Pharmacogenomics, Department of Neuroscience and Pharmacology, The Faculty of Health and Medical Sciences, University of Copenhagen , DK-2200 Copenhagen N, Denmark.
出版信息
ACS Med Chem Lett. 2014 Mar 27;5(6):696-9. doi: 10.1021/ml5000806. eCollection 2014 Jun 12.
Abstract
Novel rhodamine-labeled ligands, based on (S)-citalopram, were synthesized and evaluated for uptake inhibition at the human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) and for binding at SERT, in transiently transfected COS7 cells. Compound 14 demonstrated high affinity binding and selectivity for SERT (K i = 3 nM). Visualization of SERT, using confocal laser scanning microscopy, validated compound 14 as a novel tool for studying SERT expression and distribution in living cells.
摘要
基于（S）-西酞普兰合成了新型罗丹明标记配体，并在瞬时转染的COS7细胞中评估了其对人血清素、多巴胺和去甲肾上腺素转运体（分别为hSERT、hDAT和hNET）的摄取抑制作用以及对SERT的结合作用。化合物14对SERT表现出高亲和力结合和选择性（K i = 3 nM）。使用共聚焦激光扫描显微镜对SERT进行可视化，证实化合物14是研究活细胞中SERT表达和分布的新型工具。
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