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

开发 F-18（正电子发射体）标记的血清素衍生物，可用于抑郁症的病理生理学。

• 批准号: 13470179
• 负责人: ENDO Keigo
• 金额: $ 6.34万
• 依托单位: Gunma University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (B)
• 财政年份: 2001
• 资助国家: 日本
• 起止时间: 2001 至 2003
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-13470179/
• 关键词: PET; F-18; Tryptophan; FAMT; Brain tumor; C-11; FDG; Depression; C-11DASB; Depression; Brain tumor

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.

正电子发射断层扫描(PET)是一种提供生理过程图像的分子成像技术。正电子发射器，如F-18或C-11，其性能允许对发射正电子的放射性药物进行准确和美观的成像。其中，葡萄糖的类似物FDG是应用最广泛的，因为它在大多数肿瘤中积聚。然而，FDG也有缺点，如在大脑中的生理性摄取或一些颗粒。FAMT，F-18标记的色氨酸衍生物，仅在脑肿瘤中分布，而在正常脑组织中不分布，有助于脑肿瘤的定位或治疗后复发的诊断。据报道，5-羟色胺(5-HT)通过调节5-羟色胺转运体(5-HTT)与抑郁症有一定的关系。本研究旨在观察5-HTT及合成的C-11标记的C-DASB(N，N-二甲基-2-(2-氨基-4-氰基苯硫基)苯甲胺)在脑内的分布，为抑郁症的病理生理研究奠定基础。

项目成果

Aoki, J.: "FDG-PET for preoperative differential diagnosis between benign and malignant soft tissue masses."Skeletal Radiol.. 32. 133-138 (2003)

Aoki, J.：“FDG-PET 用于良性和恶性软组织肿块的术前鉴别诊断。”Skeletal Radiol.. 32. 133-138 (2003)

Nakayama, M.: "A new ^<68>Ge/^<68>Ga generator system using an organic polymer containing N-methylglucamine groups as adsorbent for ^<68>Ge."Applied Radiation and Isotopes. 58. 9-14 (2003)

Nakayama, M.：“一种新的 ^ 68 > Ge/^ 68 > Ga 发生器系统，使用含有 N-甲基葡糖胺基团的有机聚合物作为 ^ 68 > Ge 吸附剂。”应用辐射和同位素。

N. Sato: "MR evaluation of the hippocampus in patients with congenital malformations of the brain"Am J Neuroradiol. 22. 389-393 (2001)

N. Sato：“先天性大脑畸形患者海马的 MR 评估”Am J Neuroradiol。

T. Inoue: "Usefulness of dual-head coincidence gamma camera with thick NaI crystals for nuclear oncology: Comparison with dedicated PET camera and conventional gamma camera with thin NaI crystals"Annals of Nuclear Medicine. 15. 141-148 (2001)

T. Inoue：“具有厚 NaI 晶体的双头符合伽马相机在核肿瘤学中的实用性：与专用 PET 相机和具有薄 NaI 晶体的传统伽马相机的比较”《核医学年鉴》。

伊藤 正敏: "臨床医のためのクリニカルPET"先端医療技術研究所. 322 (2001)

伊藤正敏：《临床医生的临床 PET》，先进医疗技术研究所 322 (2001)。