ENZYME TARGETED IMAGING AGENTS FOR NEUROPSYCHIATRY

该项目涉及开发成像试剂，将使 脑内多巴胺能和5-羟色胺能活性的测定 非侵入性使用正电子发射断层扫描(PET)。短暂的 正电子发射同位素，18F(t+=110min)和11C(t+=20min)， 被引入到氨基酸类似物中，这些类似物是 多巴胺和5-羟色胺生物合成中的限速酶。 这些化合物的非放射性样品首先被合成并 用多核核磁共振(1H，11C，19F)进行了表征。此外，两者 所需化合物的前体和酶产物为 制备并用核磁共振对其进行了表征。这些前体和酶 产品用于合成所需的化合物及其 分别进行代谢特征分析。放射性标记的化合物是 然后在体外和体内评价其作为显像剂用于 帕金森氏症等神经精神障碍的研究， 情感障碍和抑郁。

This project involves developing imaging agents which will allow the asessment of dopaminergic and serotonergic activity in the brain non-invasively using positron emission tomography (PET). Short-lived positron emitting isotopes, 18F (t+=110 min.) and 11C (t+=20 min.), are introduced into amino acid analogs which are substrates of the rate limiting enzymes in the biosynthesis of dopamine and serotonin. Non-radioactive samples of these compounds are first sythesized and characterized by multinuclear NMR (1H, 11C, 19F). In addition, both the precursors and enzyme products of the desired compounds are prepared and characterized by NMR. These precursors and enzyme products are used in the synthesis of the desired compounds and their metabolic characterization, respectively. Radiolabeled compounds are then evaluated, in vitro and in vivo, as imaging agents for use in the study of neuropsychiatric disorders such as Parkinson's disease, affective disorders and depression.