Development of New Noninvasive Methods of Functional Imaging Using Biologically Active Substances Labelled with Positron Emitting Radionuclides

使用正电子发射放射性核素标记的生物活性物质开发新的无创功能成像方法

• 批准号: 04557046
• 负责人: TADA Masao
• 金额: $ 6.85万
• 依托单位: Tohoku University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Developmental Scientific Research (B)
• 财政年份: 1992
• 资助国家: 日本
• 起止时间: 1992 至 1994
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-04557046/
• 关键词: Synthesis; [fluoroacetyl-^<18>F]Fluoromelatonin; N^<omega>-[^<18>F]Fluoroacetylserotonin; RI; N-[^<18>F]Fluoroacetyl-D-glucosamine; 2-Deoxy-2-[^<18>F]fluoro-D-galactose; PET; Imaging; 診断; 陽電子放出核種; [^<18>F]フルオロアセチルグルコサミン; 標識体; アミノ糖; 腫瘍; 標識グルコ

1. Chemical ResearchAn efficient synthesis of[fluoroacetyl-^<18>F]fluoromelatonin (1) has been established. The desired isotope (1) was obtained in a 26.7% radiochemical yield. The purity, specific activity and the total time required for its synthesis are>98%, 540mCi/mmol and ca.90 min, respectively. N^<omega>-[^<18>F]Fluoroacetylserotonin (2) was also synthesized under similar conditions in 22.6% radiochemical yield. The purity and specific activity of the hormone (2) are>98% and 600mCi/mmol, respectively.2. Medical ResearchWe have examined the feasibility of positron labelled radiopharmaceuticals for functional imaging.(1). Tissue distribution of (1) has been studies using mice. The distribution was similar to that of iodolabelled melatonin which has been reported previously. It is suggested that (1)may be a useful tracer for studying the correlation of melatonin metabolism and circadian rhythm.(2). We have studied the tumor imaging with PET using N-[^<18>F]Fluoroacetyl-D-glucosamine(3). Sugar(3) was intravenously injected through the ear vein to a Japanese white rabbit bearing a VX2 tumor in the thigh, and PET imaging was performed. Tumor was clearly visualized using (3).(3) .Clinical PET sudy demonstrated the usefulness of 2-Deoxy-2-[^<18>F]fluoro-D-galactose for the detection of extrahepatic metastasis of hepatoma.

1.化学研究建立了[氟乙酰基-^<18>F]氟褪黑素（1）的有效合成方法。以26.7%的放射化学产率获得所需的同位素（1）。其纯度&gt; 98%，比活性为540 mCi/mmol，合成所需时间约90 min。在<omega><18>相似的条件下也合成了N^ -[^ F]氟乙酰羟色胺（2），放射化学产率为22.6%。激素（2）的纯度&gt;98%，比活性为600 mCi/mmol.医学研究我们已经研究了正电子标记放射性药物用于功能成像的可行性。（一）.已经使用小鼠研究了（1）的组织分布。分布与先前报道的碘标记褪黑激素的分布相似。提示：（1）可能是研究褪黑素代谢与昼夜节律相关性的一种有用的示踪剂。（二）、我们已经研究了使用N-[13 <18>F]氟乙酰基-D-葡糖胺的PET肿瘤成像（3）。通过耳静脉将糖（3）静脉注射至在大腿中携带VX 2肿瘤的日本白色兔子，并进行PET成像。使用⑶使肿瘤清楚地可视化。(3)临床PET研究证实2-脱氧-2-氟<18>代-D-半乳糖对肝癌肝外转移的检测是有效的。

项目成果

Masao Tada,Ren Iwata,Hiroshi Sugiyama et al.: "An Efficient Synthesis of N^ω-[^<18>F]-Fluoroacetylserotonin(N^ω-[^<18>F]-Fluoroacetyl‐5‐hydroxytryptamine)" J.Labelled Compds.Radiopharm.34. 741-746 (1994)

Masao Tada、Ren Iwata、Hiroshi Sugiyama 等人：“N^ω-[^<18>F]-氟乙酰血清素（N^ω-[^<18>F]-氟乙酰基-5-羟色胺）的高效合成” J.Labeled Compds.Radiopharm.34。741-746 (1994)

Kazuo Kubota: "Evaluation of the Treatment Response of Lung Cancer with Positron Emission Tomography and L-[methyl-^<11>C]Methionine:A Preliminary Study" Eur.J.Nucl.Med.20. 495-501 (1993)

Kazuo Kubota：“用正电子发射断层扫描和L-[甲基-^ 11 C]甲硫氨酸评估肺癌的治疗反应：初步研究”Eur.J.Nucl.Med.20。

Masao Tada, Ren Iwata, Hiroshi Sugiyama et al.: "A Rapid Synthesis of [fluoroacetyl-^<18>F]Fluoromelatonin(N^ω-[^<18>F]Fluoroacetyl-5-methoxy-tryptamine), a Potential Diagnostic Imaging Agent" J. Labelled Compds. Radiopharm.33. 601-606 (1993)

Masao Tada、Ren Iwata、Hiroshi Sugiyama 等人：“[氟乙酰基-^<18>F]氟褪黑素(N^ω-[^<18>F]氟乙酰基-5-甲氧基-色胺)的快速合成，一种潜在的诊断成像剂”J. Labeled Compds. Radiopharm.33. 601-606 (1993)

Takehiko Fujiwara, Kazuo Kubota, Masao Tada, Masatoshi Itoh, Tachio Sato, Ren Iwata, Kazunori Sato, Hiroshi Fukuda, and Tatsuo Ido: "N- (F-18) Fluoroacetyl-D-glucosamine : A New Positron Labeled Pharmaceutical for Cancer Study" Tohoku J.Exp.Med.168. 317-3

Takehiko Fujiwara、Kazuo Kubota、Masao Tada、Masatoshi Itoh、Tachio Sato、Ren Iwata、Kazunori Sato、Hiroshi Fukuda 和 Tatsuo Ido：“N-（F-18）氟乙酰基-D-葡萄糖胺：用于癌症研究的新型正电子标记药物

Hiromu Takahashi: "^<18>FDG Uptake of the Myocardium in PET Images of Patients under Cancer Chemotherapy" CYRIC Ann.Rep.(Tohoku Univ.). 1991. 264-267 (1992)

Hiromu Takahashi：“^18>癌症化疗患者PET图像中心肌的FDG摄取”CYRIC Ann.Rep.(东北大学)。