Radiopharmaceutical Chemistry with Iodine-124: A Non-Standard Radiohalogen for Positron Emission Tomography
Radiopharmaceutical Chemistry with Iodine-124: A Non-Standard Radiohalogen for Positron Emission Tomography
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DOI：
10.2174/157340611796799221
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发表时间：
2011-09-01
影响因子：
2.3
通讯作者：
Divgi, Chaitanya R.
中科院分区：
文献类型：
--
作者：
Chacko, Ann-Marie;Divgi, Chaitanya R.
正电子发射断层扫描（PET）是一种功能强大的分子成像技术，能够在体内和真实的时间成像和监测分子事件。随着PET放射性药物用于体内生理和病理过程成像的应用增加，需要具有更长物理和生物半衰期的多功能正电子发射体。传统的PET放射性核素，如碳-11（C-11）和氟-18（F-18），半衰期相对较短（分别为20分钟和110分钟）。在目前可用的正电子发射体中，非标准放射性卤素碘-124（I-124）具有最长的物理半衰期，为4.2天。这一点，结合放射性碘的放射化学特性，有助于提高I-124在临床核医学和小动物PET成像研究中研究缓慢而复杂的药代动力学过程的效用。本文将从碘-124的制备开始，综述碘-124作为正电子发射核素用于分子成像的潜力。特别强调将放在基本的放射化学，因为它适用于各种I-124标记的化合物的生产，从小分子，生物分子，如肽和蛋白质，最后到大分子，如纳米粒子。最后，该综述将强调未来使用I-124作为PET放射化学和分子成像中的正电子发射体的有前途的方向。
Positron emission tomography (PET) is a powerful molecular imaging technology with the ability to image and monitor molecular events in vivo and in real time. With the increased application of PET radiopharmaceuticals for imaging physiological and pathological processes in vivo, there is a demand for versatile positron emitters with longer physical and biological half-lives. Traditional PET radionuclides, such as carbon-11 (C-11) and fluorine-18 (F-18), have relatively short half-lives (20 min and 110 min, respectively). Among the currently available positron emitters, the non-standard radiohalogen iodine-124 (I-124) has the longest physical half-life at 4.2 d. This, combined with the well characterized radiochemistry of radioiodine, is contributing to the increasing utility of I-124 in investigating slow and complex pharmacokinetic processes in clinical nuclear medicine and small animal PET imaging studies. This review will summarize the progress to date on the potential of I-124 as a positron emitting nuclide for molecular imaging purposes, beginning with the production of I-124. Particular emphasis will be placed on the basic radiochemistry as it applies to the production of various I-124-labeled compounds, from small molecules, to biomolecules such as peptides and proteins, and finally to macromolecules like nanoparticles. The review will conclude by highlighting promising future directions in using I-124 as a positron emitter in PET radiochemistry and molecular imaging.