2001 Fiscal Year Final Research Report Summary
Development of Tc-99m labeled long chain fatty acid derivative for myocardial imaging
| Project/Area Number |
12670866
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 一般 |
|---|
| Research Field |
Radiation science
|
|---|
| Research Institution | Kyoto University |
|---|
Principal Investigator |
MAGATA Yasuhiro Kyoto University, Graduate School of Pharmaceutical Sciences, Associate Professor, 薬学研究科, 助教授 (20209399)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
TADAMURA Eiji Kyoto University, Graduate School of Medicine, Assistant Professor, 医学研究科, 助手 (70303831)
|
|---|
| Project Period (FY) |
2000 – 2001
|
| Keywords | Long chain fatty acid / Tc-99m / SPECT / RAT / Myocardium / Radiopharmaceuticals / Diagnosis |
|---|
| Research Abstract |
C-11 and I-123 labeled long chain fatty acid derivatives have been reported as useful radiopharmaceuticals 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. After the synthesis, Tc-99m labeling was performed by ligand-exchange reaction with Tc-99m-pertechnetate reduced by Sn(II) glucoheptonate in diluted ethanol solution and purified with HPLC system. Tc-99m labeled long chain fatty acid derivatives were obtained with radiochemical yield of >70 % and radiochemical purity of >95 %.
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). Beta oxidation of Tc-99m-MAMA-HDA was investigated using primary cell culture of adult rats myocardium as a preliminary study. The metabolites were analyzed by radio TLC. It was indicated that Tc-99m-MAMA-HDA was metabolized to a short chain fatty acid derivative by the myocardium in vitro.
In conclusion, Tc-99m-MAMA-HDA may be recognized as a long chain fatty acid in the myocardium although further examination are required. This Tc-99m labeled compound is useful to evaluate fatty acid metabolism in the myocardium.
|
Research Products
(8 results)
