TECHNETIUM-99M LABELED FATTY ACID ANALOGS FOR IMAGING

这项拟议的研究计划的目标是开发一种广泛的 检测患者心肌代谢变化的临床试剂 99m标记脂肪的单光子发射计算机断层扫描技术 本申请中提出的酸类。拟议的研究将确定 ~(99m)Tm标记脂肪酸的最佳结构特征 核医学心肌显像剂的研制。TC-99M标记 脂肪酸将被合成，并在大鼠的心肌中研究其摄取。 ~(99m)Tc标记的三个系列脂肪酸的不同位置 关于亲脂和羧基的位置将被制备，并且它们的 其化学结构由其Re类似物的制备所鉴定。这些 脂肪酸类似物利用1，2-二硫-5，8-二氮杂环十烷和 ‘3+1’原则作为锶的螯合部分。它们被设计成 长链脂肪酸载体蛋白进入心肌细胞的研究 天然脂肪酸使用的机制。脂肪酸的衍生品将是 设计成它们不能完全被分解。以这种方式 示踪剂被捕获后，运输/传递和新陈代谢可以成像 在细胞内。这些研究将确定这类人的潜力 评价脂肪酸地区差异的放射性药物 发生在缺血性心脏病和心肌病中的代谢。 建议的商业应用：不可用

The objective of this proposed research plan is to develop a widespread clinical agent for detecting myocardial metabolic changes in patients using single photon emission computed tomography and technetium99m labeled fatty acids proposed in this application. The proposed research will determine the optimal structure features of technetium-99m labeled fatty acid for the development of a myocardial imaging agent for nuclear medicine. Tc-99m-labeled fatty acids will be synthesized and their myocardium uptake studied in rats. Three series of fatty acids labeled with Tc-99m at different positions with respect to the lipophilic and carboxylic sites will be prepared and their chemical structure identified by preparation of their rhenium analogs. These fatty acid analogs utilize both the 1,2-dithia-5,8-diazacyclodecan and the '3+1' principle as the technetium chelating moieties. They are designed to be transported into myocardial cells by the long chain fatty acid carrier protein mechanism used by natural fatty acids. The fatty acid derivatives will be designed such that they cannot be completely catabolized. In this manner transport/delivery and metabolism can be imaged after the tracer is 'trapped' intracellularly. These studies will determine the potential of this class of radiopharmaceuticals for evaluation of region discrepancies in fatty acid metabolism which occur in ischemic heart disease and cardiomyopathies. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE