Radiochemical methods for labeling and isotope production

标记和同位素生产的放射化学方法

• 批准号: RGPIN-2021-03848
• 负责人: Campbell, Michael
• 金额: $ 1.75万
• 依托单位: Lakehead University
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2021
• 资助国家: 加拿大
• 起止时间: 2021-01-01 至 2022-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=742749
• 关键词: Radiochemical; methods; labeling; isotope; production

This research program is focused on the development of new methods for the cyclotron production of radionuclides and developing reactions and tools to improve access to radionuclides for use in research, industry and health care. During the course of this research we will develop and show the application of solid phase labeling methods using F-18 fluoride and C-11 carbon for the labeling of molecules of biological interest. We will also use the neutron flux produced by a cyclotron during routine isotope production to create short-lived beta emitters via neutron activation that can be used for research and analysis. Application of Solid Phase Synthesis (SPS) Methods to Radiolabeling When introducing a radionuclide into a small molecule or protein for labeling as an imaging probe you are working against the clock. The isotope is always decaying so time spent performing the synthesis and purifying the product will negatively impact the yield of the tracer. Many of these reactions require some purification step to remove excess reagents and catalysts. This research program will develop SPS reagents and procedures to minimize reaction time and work to reduce the purification requirements. In radiochemistry the molecule to be labeled and reagents are in a large excess with respect to the radionuclide. This helps to ensure that most of the radionuclide reacts, it can also pose a challenge for separating the labeled product from the excess reagents. This portion of the program is focused on preparing "react and release" resins where the substrate to be labeled is immobilized on solid support and is only released on reaction with F-18. Cyclotron Neutron Activation The ability of cyclotrons to produce short lived PET radionuclides has been well established. What is significantly more difficult is the production of neutron rich beta emitters. Most often neutron activation requires access to a reactor-based neutron source. Unfortunately, space in research reactors is limited and can be costly, particularly with only a limited number of research reactors in Canada. There are, however, a growing number of medical cyclotrons available across the country. These cyclotrons typically are running on a regular, often daily, basis producing isotopes such as 18F for imaging. This research will leverage the neutron flux from routine cyclotron production runs for the irradiation of samples for mineral analysis. The application of this technique will allow access to radionuclides with very sort half-lives (T1/2 < 1 day) for research that shipping times would otherwise make inaccessible. Neutron activation will also be applied to the analysis of mineral samples. This will allow for now destructive, high throughput analysis of mineral, bullion and waste streams from the mining industry to identify metals such as gold, silver and the platinum group elements.

这一研究方案的重点是开发回旋加速器生产放射性核素的新方法，并开发反应和工具，以改善用于研究、工业和保健的放射性核素的获取。在本研究过程中，我们将开发并展示使用F-18氟化物和C-11碳的固相标记方法的应用，用于标记生物学感兴趣的分子。我们还将利用回旋加速器在常规同位素生产过程中产生的中子通量，通过中子激活来创建可用于研究和分析的短寿命β发射器。固相合成（SPS）方法在放射性标记中的应用当将放射性核素引入小分子或蛋白质中作为成像探针进行标记时，您需要争分夺秒。同位素总是在衰变，所以花在合成和纯化产物上的时间会对示踪剂的产率产生负面影响。许多这些反应需要一些净化步骤来去除多余的试剂和催化剂。该研究计划将开发SPS试剂和程序，以最大限度地减少反应时间和工作，以减少净化要求。在放射化学中，要标记的分子和试剂相对于放射性核素是大量过剩的。这有助于确保大多数放射性核素发生反应，但也可能对将标记产物与多余试剂分离提出挑战。该计划的这一部分侧重于制备“反应和释放”树脂，其中要标记的基材固定在固体载体上，并且仅在与F-18反应时释放。回旋加速器中子活化回旋加速器产生短寿命PET放射性核素的能力已经得到了很好的证实。更困难的是产生富含中子的发射体。大多数情况下，中子激活需要使用基于反应堆的中子源。不幸的是，研究堆的空间是有限的，而且可能是昂贵的，特别是在加拿大只有有限数量的研究堆。然而，全国各地有越来越多的医用回旋加速器可供使用。这些回旋加速器通常定期运行，通常每天运行，产生用于成像的18F等同位素。本研究将利用常规回旋加速器生产运行的中子通量辐照样品进行矿物分析。这项技术的应用将使研究人员能够获得半衰期非常短的放射性核素（T1/2 < 1天），否则运输时间将无法获得这些放射性核素。中子活化也将应用于矿物样品的分析。这将允许对来自采矿业的矿物、金条和废物流进行破坏性的高通量分析，以识别金、银和铂族元素等金属。