Novel hydrophilic Silicon-Fluoride-Acceptors (SiFAs) for in vivo Positron Emission Tomography (PET)

该建议旨在解决正电子发射断层扫描（PET）昂贵且很少使用的主要问题，尽管该方法对从癌症到神经病学和心脏病学等多种疾病的患者预后都很重要。PET依赖于一种叫做放射性示踪剂的造影剂。这些放射性示踪剂的合成既昂贵又复杂，需要专家在设备昂贵的实验室里工作。在过去的几年里，人们发现了一种以更简单、更便宜的方式获得放射性示踪剂的可能途径。然而，第一个合成子（虽然很容易标记）在放射性示踪剂的合成中没有成功，因为由于它们的化学性质，它们改变了放射性示踪剂的亲脂性，从而改变了体内行为。这个建议包含了一个系统的研究，如何改变这种亲脂性，导致放射性示踪剂达到他们的目标。一旦确定了最佳结构，长期目标将是使生产过程自动化，并符合GMP要求，最终生产出可商用的产品，使每个拥有核医学技术人员的医院或诊所都能生产廉价高效的放射性示踪剂。如果成功，这笔拨款将使患者更好地获得PET扫描，因为它们对公共卫生保健系统来说更便宜，而且不需要那么多高素质的人员来实现它们。

This proposal aims to solve the main problem causing Positron Emission Tomography (PET) to be expensive and rarely used, although the methodology is important for patient outcome in a large variety of diseases, from cancer to neurology and cardiology. PET is dependend on contrast agents called radiotracers. The synthesis of these radiotracers is expensive and complex, requiring specialists working in expensively equipped laboratories.During the last years, a possible pathway to obtain radiotracers in a much simpler and therefore cheaper fashion was found. However, the first synthons (although easy to label) were not successful in the synthesis of radiotracers because due to their chemical nature, they changed the lipophilicity of the radiotracers, and thus the in vivo behavior. This proposal contains a systematic study of how this lipophilicity can be altered, leading to radiotracers reaching their targets. Once the best structure has been identified, the long-term goal would be to automate the production process with GMP compliance to ultimately come up with a commercially available product, allowing every hospital or clinic with nuclear medicine technicians to produce cheap and efficient radiotracers.If successful, this grant will lead to a better access of patients to PET scans, since they will be less expensive for the public Health Care system, and less highly qualified personnel is needed to make them feasible.