Development of F-18 (positron emitter) labeled serotonin derivatives useful for the pathophysiology of depression.

正电子发射断层扫描（PET）是一种分子成像技术，可以提供生理过程的图像。正电子发射体如F-18或C-11具有允许发射正电子的放射性药物的准确和美丽的成像的性质。其中，葡萄糖的类似物FDG是最广泛使用的，因为它在大多数肿瘤中积累。然而，FDG也有缺点，例如在大脑中的生理摄取或一些颗粒化。FAMT是F-18标记的色氨酸衍生物，仅在脑肿瘤中分布，而在正常脑中不分布，对脑肿瘤的定位或治疗后复发的诊断有重要意义。5-羟色胺（5-HT）通过调节5-HT转运体（5-HTT）与抑郁症的发生有关，本研究拟观察5-HTT在脑内的分布，并合成了C-11标记的5-<11>C-DASB（N，N-二甲基-2-（2-氨基-4-氰基苯硫基）<11>苄胺），为研究抑郁症的病理生理机制提供了新的材料。

Positron emission tomography (PET) is a molecular imaging technique that provides images of physiological process. The positron emitters such as F-18 or C-11 have properties which permit accurate and beautiful imaging of positron-emitting radiopharmaceuticals. Among them, FDG, an analogue of glucose, is the most widely used, since it accumulates in the most tumors. However FDG has drawbacks, such as the physiological uptake in the brain or some granulations. FAMT, F-18 labeled derivative of tryptophan, distribute only in the brain tumor, but not in the normal brain, and is useful for the localization of brain tumor or the diagnosis of the recurrence after therapy. It is reported that serotonin (5-HT) has some relation with depression, by regulating the serotonin transporter (5-HTT).In the present study, we intended to visualize the brain distribution of 5-HTT and synthesized C-11 labeled ^<11>C-DASB (N,N-dimethyl-2-(2-amino-4-cyanophenylthio) benzyl-amine ^<11>C-DASB and seemed to be useful for studying the pathophysiology of depression.