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

这项建议旨在解决导致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学和心脏病学的各种疾病的患者预后非常重要。PET依赖于称为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，需要在装备昂贵的实验室中工作的专家。**在过去的几年里，人们找到了一种可能的途径，以一种更简单、更便宜的方式获得放射性示踪剂。然而，第一个合成子(尽管很容易标记)在合成放射性示踪剂方面并不成功，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。这项提议包含了一项关于如何改变这种亲脂性，从而导致放射性示踪剂到达目标的系统研究。一旦确定了最佳结构，长期目标将是在符合GMP的情况下实现生产过程的自动化，最终提出一种商业可用产品，使每一家拥有核医学技术人员的医院或诊所都能生产廉价而高效的放射性示踪剂。**如果成功，这笔赠款将使患者更容易获得PET扫描，因为对公共卫生保健系统来说，这将是更便宜的扫描，而不需要高素质的人员来使其可行。

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.