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Development of Tc-99m labeled long chain fatty acid derivative for myocardial imaging.

开发用于心肌成像的 Tc-99m 标记的长链脂肪酸衍生物。

基本信息

批准号：
14570853
负责人：
MAGATA Yasuhiro
金额：
$ 2.24万
依托单位：
HAMAMATSU UNIVERSITY SCHOOL OF MEDICINE
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2002
资助国家：
日本
起止时间：
2002 至 2003
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-14570853/
关键词：
Branched Fatty Acid Tc-99m SPECT Rat Diagnosis Radiopharmaceutical Myocardial Function

项目摘要

C-11 and I-123 labeled long chain fatty acid derivatives have been reported as useful radiopharjnaceuticals for estimation of myocardial fatty acid metabolism. We have reported that ^<99m>Tc-MAMA-HA, middle chain fatty acid derivative, is metabolized by beta-oxidation in a liver and MAMA ligand is useful to attach to the omega-position of fatty acid derivative as a chelating group with Tc-99m. Based on these findings, we focused on developing Tc-99m labeled long chain fatty acid derivative that reflected fatty acid metabolism in the myocardium. We synthesized some long chain fatty acids (carbon length ; 11 (MAMA-DA), 15 (MAMA-HDA)) containing MAMA group in its molecule as a chelating group with Tc-99m. Then, Tc-99m labeling and biodistribution studies were performed. A higher initial uptake of Tc-99m-MAMA-HDA was observed in in vivo animal experiments using mice. The value was half of that by I-125-IPPA (p-iodo-phenyl pentadecanoic acid). β-oxydative metabolite, short chain fatty acid … More derivative, Tc-99m-MAMA-BA was found in urine post-injection of Tc-99m-MAMA-HDA in normal rats. These results showed that Tc-99m-MAMA-HDA was recognized as a long chain fatty acid in the body. β-branched long chain fatty acid derivative, such as I-123-BMIPP, is used in clinical nuclear medicine. The radioactivity is accumulated in the heart by so-called metabolic trapping mechanism and this biological character is very useful for routine use. Then, synthesis of Tc-99m-MAMA-β-methyl-FA was carried out and an expected precursor, Trityl-MAMA-β-methyl-HDA was obtained with 14 steps. After Tc-99m labeling of this new compound, apreliminal biodistribution study was performed in normal mice. Although the radioactivity in the heart was not retained, further investigations may be needed. On the other hand, energy metabolism in the heart of Dahl model rats was investigated using an animal PET scanner and FDG. We established the experimental system and found usefulness of nuclear medicine technique in this field. Less

已报道C-11和I-123标记的长链脂肪酸衍生物是用于估计心肌脂肪酸代谢的有用的放射性药物。我们已经报道了<99m>，中链脂肪酸衍生物-基于这些发现，我们专注于开发反映心肌中脂肪酸代谢的Tc-99 m标记的长链脂肪酸衍生物。我们合成了一些长链脂肪酸（碳长11（MAMA-DA），15（MAMA-HDA）），其分子中含有MAMA基团作为与Tc-99 m的螯合基团。然后，进行Tc-99 m标记和生物分布研究。在使用小鼠的体内动物实验中观察到较高的Tc-99 m-MAMA-HDA初始摄取。该值是I-125-IPPA（对碘苯基十五烷酸）的一半。β-氧化代谢产物，短链脂肪酸 ...更多信息正常大鼠注射Tc-99 m-MAMA-HDA后，尿中有Tc-99 m-MAMA-BA。这些结果表明，Tc-99 m-MAMA-HDA在体内被识别为长链脂肪酸。β-支链长链脂肪酸衍生物，如I-123-BMIPP，用于临床核医学。放射性通过所谓的代谢捕获机制在心脏中积累，这种生物学特性对于常规使用非常有用。在此基础上，进行了Tc-99 m-MAMA-β-methyl-FA的合成，经过14步反应得到了预期的前体Trityl-MAMA-β-methyl-HDA。用~（99）Tc-m标记该化合物后，在正常小鼠体内进行了生物分布的初步研究。虽然心脏中的放射性未保留，但可能需要进一步研究。另一方面，使用动物PET扫描仪和FDG研究Dahl模型大鼠心脏中的能量代谢。我们建立了实验系统，发现了核医学技术在这一领域的应用价值。少