Department of Neuroimaging and Interventional Radiology (NI & IR), National Institute of Mental Health and Neurosciences (NIMHANS), Bengaluru, India.
National Institute of Mental Health, National Institutes of Health, Bethesda, MD, USA.
Expert Opin Ther Pat. 2022 Jul;32(7):817-831. doi: 10.1080/13543776.2022.2070003. Epub 2022 Apr 28.
Carbon-11 is a short-lived radionuclide with versatile applications in synthetic methodologies to develop a variety of novel PET radiotracers. Different primary and secondary carbon-11 precursors are generated from cyclotron produced [C]CO and used to insert carbon-11 radionuclide into the target-specific bioactive molecules.
In this review, the patents as well as specific research articles on carbon-11 radiotracer synthesis and PET imaging applications in various diseases are mentioned since 2012 to 2022 through SciFinder database.
Carbon-11 is generally easier to insert into more organic scaffolds as a greater variety of functional groups. Despite the short half-life of carbon-11 radionuclide ( = 20.4 min), it is widely used in PET radiotracer development due to its direct insertion into bioactive compounds and less isotopic dilution unlike other positron emitters like fluorine-18. Various synthons can be easily generated using the primary and secondary carbon-11 precursors . The carbon-11 radiotracers provide target-oriented information associated with the pharmacology, and physiological conditions of the disease status. Various protocols and automated methods were adapted for easy and convenient synthesis of carbon-11 radiotracers. The PET advances drug development and clinical trials by revealing biological target engagement, proof of mechanism, pharmacokinetic, and pharmacodynamic profiles of new drug candidates using selective radiotracers.
碳-11 是一种短寿命的放射性核素，在合成方法学中有多种应用，可开发出各种新型正电子发射断层扫描（PET）放射性示踪剂。不同的初级和次级碳-11 前体由回旋加速器产生的 [C]CO 生成，并用于将碳-11 放射性核素插入到针对特定生物活性分子的靶标中。
本文通过 SciFinder 数据库，综述了 2012 年至 2022 年间有关碳-11 放射性示踪剂合成以及在各种疾病中的 PET 成像应用的专利和特定研究文章。
碳-11 通常更容易插入到更多的有机支架中，因为它具有更多种类的功能基团。尽管碳-11 放射性核素（t1/2=20.4 分钟）的半衰期较短，但由于它可以直接插入到生物活性化合物中，与其他正电子发射体（如氟-18）相比，同位素稀释较少，因此在 PET 放射性示踪剂的开发中得到了广泛应用。可以使用初级和次级碳-11 前体很容易地生成各种合成子。碳-11 放射性示踪剂提供与疾病状态的药理学和生理学相关的靶向信息。已经采用了各种方案和自动化方法来方便、便捷地合成碳-11 放射性示踪剂。通过使用选择性放射性示踪剂揭示新候选药物的生物靶标结合、机制证明、药代动力学和药效动力学特征，PET 推动了药物开发和临床试验。
