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<^(19)F> NMR Study of Fluorinated Compounds in vivo with a view to Medical Application.

氟化化合物的体内<^(19)F> NMR研究以用于医学应用。

基本信息

批准号：
59460194
负责人：
KOJIMA Masaharu
金额：
$ 4.93万
依托单位：
Kyushu University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (B)
财政年份：
1984
资助国家：
日本
起止时间：
1984 至 1986
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-59460194/
关键词：
F-19 NMR NMR Imaging of hetero nucleus F-compound In vivo Dynamics Glucose metabolism 2-Deoxy-2-fluoro-D-hexose FDG 麻酔剤

项目摘要

1. The purpose of this project is a basic in vivo biochemical study of fluorine compounds including fluorine containing pharmaceuticals with a view to medical application by the use of F-19 NMR.2. We succeeded in the construction of a F-19 NMR chemical shift image with a phantom consists of inhalation aneshetics, halothane and methoxyflurane, adsorbed to the lipid dispersions as a model of brain.3. We developed new, improved synthetic methods of fluorine compounds including 2-deoxy-2-fluoro-D-glucose(FDG) a pharmaceutical used for the monitoring of glucose utilization, 2-deoxy-2-fluoro-D-mannose(FDM), and 2-deoxy-2-fluoro-D-galactose.4. The metabolic fate of FDG was studied in mice with excised organs by F-19 NMR. It was found that FDG injected to mice was converted to FDM(or FDM-6-phosphate) in vivo. The reaction was proved to be reversible by FDM injection, i.e., FDG is accumulated in tissues in the form of FDG-6-phos-phate and FDM-6-phosphate. The previous concept of FDG trapping mechanism at the site of high glucose metabolism was revised by this study.5. The F-19 NMR images of FDG and FDGal were made from a slice of brain and a whole body of mice with the concentrations of fluorinated hexose of 2 - 3 mM or less. Although the contrast and the resolution of these images were not satisfactory at the present stage, the present result gives a strong promise to the future development of this method.6. We hope to continue this project by the employment of F-19 imaging system at high magnetic field.

1.该项目的目的是利用F-19 NMR对氟化合物（包括含氟药物）进行基本的体内生物化学研究，以期将其用于医学应用。我们成功地构建了一个F-19 NMR化学位移图像与体模组成的吸入麻醉剂，氟烷和甲氧氟醚，吸附到脂质分散体作为一个模型的大脑.我们开发了新的、改进的含氟化合物的合成方法，包括用于监测葡萄糖利用的药物2-脱氧-2-氟-D-葡萄糖（FDG）、2-脱氧-2-氟-D-甘露糖（FDM）和2-脱氧-2-氟-D-半乳糖.通过F-19 NMR研究了具有切除器官的小鼠中FDG的代谢命运。发现注射给小鼠的FDG在体内转化为FDM（或FDM-6-磷酸）。通过FDM注射证明该反应是可逆的，即，FDG以FDG-6-磷酸盐和FDM-6-磷酸盐的形式在组织中积累。本研究修正了以往关于高糖代谢部位FDG捕获机制的概念.在氟代己糖浓度为2 - 3 mM或更低的条件下，对小鼠脑片和全身进行了FDG和FDGal的F-19 NMR成像，虽然目前这些图像的对比度和分辨率还不令人满意，但本研究结果为该方法的发展提供了有力的保证.我们希望通过在强磁场下使用F-19成像系统来继续这一项目。