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开发F-标记的性水性转化环氧 octene 作为PET探头构造的生物直角工具

Muyun Xu¹, Xinrui Ma¹, Jessica E Pigga²

¹Department of Radiology, Biomedical Research Imaging Center, and Lineberger Comprehensive Cancer Center, the University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, 27599, USA. zhanhong_wu@med.unc.edu.

Chemical communications (Cambridge, England)

|October 25, 2023

概括

研究人员开发了一种新的水友性-18标记化合物,[18F]3,用于PET成像. 这种多功能的追踪器可以快速创建各种小分子,,蛋白质和基于人体的成像探针.

科学领域:

放射化学放射化学是指辐射化学.
分子成像学分子成像学
生物技术是生物技术.

背景情况:

pozitron发射断层扫描 (PET) 成像依赖于开发新的放射标记物.
有效和多用途的放射性标记方法对于扩大PET应用至关重要.
对于改善药物动力学特性和减少非特异性吸收,水友性痕迹剂是可取的.

研究的目的:

开发一种用于PET成像的新型水友性-18标记型标记物 ([18F]3).
为了证明[18F]3在构建各种PET成像剂中的实用性.
建立一个简单的放射性化方法,以快速开发探头.

主要方法:

合成一种水友性α-三级-乙烯 (a-TCO) 衍生物前体.
单阶段的放射性化反应产生[18F]3.3.
通过[18F]3.3.使用各种小分子,,蛋白质和基于diabody的成像探针的并行合成.

主要成果:

成功开发了一种具有logP值为0.28.3的亲水性[18F]3追踪器.
在单阶段放射性化中达到高达52%的放射性化学产量 (RCY).
证明了多种PET成像剂的并行构建,包括小分子,,蛋白质和糖尿病体.

结论:

开发的[18F]3追踪器是PET成像探头开发的多功能和高效工具.
单阶段放射性化方法允许快速生成各种放射性标记剂.
这种方法显著扩大了为各种生物目标创建定制PET成像剂的工具包.

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