BETA-ADRENERGIC LIGANDS FOR PET--SYNTHESIS AND TESTING

描述：(改编自应用程序)测量 β-肾上腺素能受体的数量和活性在 对心脏病及其治疗的评价。拟议的工作将 重点开发高亲和力的β受体配体 他们期望获得高质量正电子断层扫描(PET)的能力 数据。这些将用碳-11和氟-18标记，使用一般 和高效的分支方法。它们的特异性受体结合 将在小鼠和猪身上测量配体，并将进行成像实验 在猪身上表演。这项工作将提供所需的数据以获得 批准将来在人体试验中使用这些示踪剂。这项工作将 还包括动力学分析，以确定使用这些工具的可行性 心脏受体定量测定的配基。如果是测试版 受体定量被证明是可行的，调查人员将进行 体内PET受体的定量测量并与 使用相同的组织进行体外测定。

DESCRIPTION: (Adapted from the application) The ability to measure the number and activity of beta-adrenergic receptors would be of value in the evaluation of heart disease and its treatment. The proposed work will focus on the development of high-affinity beta receptor ligands chosen for their expected capacity to yield good quality positron tomographic (PET) data. These will be labeled with carbon-11 and fluorine-18 using a general and efficient branching approach. The specific receptor binding of these ligands will be measured in mice and pigs, and imaging experiments will be performed in pigs. This work will provide the needed data for obtaining approval for future use of these tracers in human subjects. This work will also include kinetic analysis to determine the feasibility of using these ligands for quantitative receptor determinations in the heart. If beta receptor quantitation proves to be feasible, the investigators will perform quantitative PET receptor measurements in vivo and compare these with in-vitro determinations using the same tissue.