亲水性 F 标记的反式-5-氧代碳烯（oxoTCO）用于高效构建正电子发射断层扫描（PET）显像剂，以提高神经降压素受体（NTR）显像的肿瘤与背景比。
Hydrophilic F-labeled trans-5-oxocene (oxoTCO) for efficient construction of PET agents with improved tumor-to-background ratios in neurotensin receptor (NTR) imaging.
机构信息
Department of Radiology and Biomedical Research Imaging Center, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, USA.
出版信息
Chem Commun (Camb). 2019 Feb 21;55(17):2485-2488. doi: 10.1039/c8cc09747j.
Abstract
An 18F-labeled trans-5-oxocene (oxoTCO) that is used to construct a PET probe for neurotensin receptor (NTR) imaging through tetrazine ligation is described here. PET probe construction proceeds with 70% RCY based on 18F-oxoTCO and is completed within seconds. The in vivo behaviour of the oxoTCO based PET probe was compared with those of analogous probes that were prepared from 18F-labeled s-TCO and d-TCO tracers. The hydrophilic 18F-oxoTCO probe showed a significantly higher tumor-to-background ratio while displaying comparable tumor uptake relative to the 18F-dTCO and 18F-sTCO derived probes.
摘要
这里描述了一种 18F 标记的反式-5-氧杂环癸烷（oxoTCO），它被用于通过四嗪连接构建用于神经降压素受体（NTR）成像的 PET 探针。基于 18F-oxoTCO，PET 探针的构建以 70%的 RCY 进行，并在几秒钟内完成。基于 oxoTCO 的 PET 探针的体内行为与那些从 18F 标记的 s-TCO 和 d-TCO 示踪剂制备的类似探针进行了比较。亲水性的 18F-oxoTCO 探针显示出明显更高的肿瘤与背景比，同时与源自 18F-dTCO 和 18F-sTCO 的探针相比，显示出相当的肿瘤摄取。
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