BETA ADRENERGIC LIGANDS FOR PET--SYNTHESIS & 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将在 评估心脏病及其治疗。 拟议的工作将 专注于开发高亲和力β受体配体， 他们的预期能力，以产生高质量的正电子断层扫描（PET） 数据 这些将被标记为碳-11和氟-18使用通用的 和有效的分支方法。 这些特异性受体结合 配体将在小鼠和猪中进行测量，成像实验将在 在猪身上进行。 这项工作将提供所需的数据， 批准这些示踪剂在人类受试者中的未来使用。 这项工作将 还包括动力学分析，以确定使用这些 用于心脏中定量受体测定的配体。 如果β 受体定量证明是可行的，研究人员将进行 体内定量PET受体测量，并将其与 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.