心血管疾病是危害人类健康的疾病之一，实现心血管疾病的早期诊断对疾病的治疗具有重大意义，在临床上成功运用放射性核素标记的显像剂来评价心肌的功能。脂肪酸心肌代谢显像剂可用于诊断心肌衰弱及心肌局部缺血，进而判断心肌细胞的活性。本论文的主要工作如下： 1、设计并合成了47个化合物，其中包括25个不同长链结构的99mTc标记的长链脂肪酸心肌代谢显像剂的前体化合物和22个相对应的Re配合物，对化合物的结构进行了鉴定和表征，Re配合物的纯度均大于95%。 2、制备了19个放射性99mTc标记的长链脂肪酸，进行了初步的评价实验。实验结果显示这一系列放射性配合物都是稳定的、脂溶性的化合物。这些放射性配合物具有心肌初始摄取值和心/血比值较高的优点，随着碳链长度的增加，放射性配合物在心肌中的滞留呈现延长的趋势。在含苯环类的长链脂肪酸配合物中，[99mTc]3.5b表现出最优的生物学性质，初始心肌摄取可达9.59±0.15%ID/g，[99mTc]3.5b的血清除较快，在5 min时心/血比达5.12，[99mTc]3.5c在60 min时心肌摄取仍可达1.43±0.05%ID/g。体内代谢实验结果表示[99mTc]3.5b在体内通过β-氧化的方式进行代谢，苯环的引入可起到阻断β-氧化的作用，进而延长心肌滞留。在尿液中，可检测到代谢产物的特征峰，说明代谢产物可通过尿液排出体外。首次合成了二酸类长链脂肪酸配合物[99mTc]4.6g，它的血清除较快(血1min/血60min = 31.97)，但是肺摄取比较高，该放射性配合物的心肌摄取及滞留均不理想，但可为脂肪酸心肌代谢显像剂的研发提供一种新的思路。

Cardiovascular disease is one that endangers people’s health. Early diagnosis of cardiovascular disease is of great significance for the treatment. In the clinical, radioactive nuclide labeled fatty acid for myocardial metabolism imaging agents are used to evaluate myocardial function. Myocardial metabolism imaging agents can be used in the diagnosis of myocardial ischemia and amyocardia to evaluate the activity of myocardial cells. The main achievements are described as follows: 1. Forty-seven compounds were designed and synthesized, including twenty-five precursors and twenty-three corresponding rhenium labeled compounds. The structure of all compounds was identified. The purity of rhenium labeled compounds was more than 95%. 2. Nineteen 99mTc-labeled fatty acid derivatives were synthesized, and the preliminary biological evaluations were carried. The results showed that those 99mTc-labeled compounds were stable and lipophilic. Those 99mTc-labeled compounds presented high initial myocardial uptake and heart/blood ratio. The myocardial retention of 99mTc-labeled compounds exhibited slowly prolonged along with the increase of carbon chain length. [99mTc]3.5b showed optimal biological characteristics. [99mTc]3.5b displayed high initial myocardial uptake of 9.59±0.15% ID/g at 1 min after injection, and myocardial uptake of 1.43±0.05%ID/g at 60 min after injection. The heart/blood ratio of [99mTc]3.5b was 5.12 at 5 min after injection. The results of metabolic experiment presented that [99mTc]3.5b may be metabolited through β-oxidation in tissue. A phenyl group (with the aromatic properties) was introduced to the γ-position of the chain to impede β-oxidation of 99mTc-labeled fatty acid and prolong myocardial retention. The radiometabolite was eliminated into the urine. In addition, compound [99mTc]4.6g was synthesized for the first time, fortunately the blood clearance was fast (blood1min/blood60min = 31.97). The myocardial uptake, retention and lung uptake of [99mTc]4.6g were not ideal, however it provided a new thought for the design of myocardial metabolism imaging agents.