Development of carbon-11 labelled PET tracers-radiochemical and technological challenges in a historic perspective
Development of carbon-11 labelled PET tracers-radiochemical and technological challenges in a historic perspective
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DOI：
10.1002/jlcr.3258
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发表时间：
2015-03-01
影响因子：
1.8
通讯作者：
Antoni, Gunnar
中科院分区：
文献类型：
--
作者：
Antoni, Gunnar
正电子发射断层扫描 (PET) 从主要研究机构专有且昂贵的研究工具，发展成为世界上大多数主要医院的临床有用模式，很大程度上取决于 40 至 50 年前开始 PET 职业生涯的一些先驱研究人员所取得的放射化学和合成技术成就。特别是，[C-11]甲基碘的引入导致了 PET 示踪剂开发历史上的巨大飞跃，能够顺利标记多种有用的示踪剂。最近且仍具有挑战性的方法学改进是过渡金属介导的 C-11-羰基化，其具有巨大的合成潜力，但尚未在临床环境中实现。这篇小型评论重点关注碳 11 放射化学和相关技术发展的历史以及其在 PET 示踪剂开发中所发挥的作用，特别强调内源性化合物的放射性标记。将提供几个例子，说明如何利用同一分子中不同位置的位置特异性标记的概念，使用放射性标记的内源性物质提供体内生物化学的基本信息。
The development of positron emission tomography (PET) from being an exclusive and expensive research tool at major research institutes to a clinically useful modality found at most major hospitals around the world is largely dependent on radiochemistry and synthesis technology achievements by a few pioneer researchers starting their PET careers 40 to 50years ago. Especially, the introduction of [C-11]methyl iodide resulted in a quantum jump in the history of PET tracer development enabling the smooth labelling of a multitude of useful tracers. A more recent and still challenging methodological improvement is transition metal mediated C-11-carbonylations, having a large synthetic potential that has, however, not yet been realized in the clinical setting. This mini-review focuses on the history of carbon-11 radiochemistry and related technology developments and the role this played in PET tracer developments, especially emphasizing radiolabelling of endogenous compounds. A few examples will be presented of how the use of radiolabelled endogenous substances have provided fundamental information of in vivo biochemistry using the concept of position-specific labelling in different positions in the same molecule.