99mTc(CO)3-15-[N-(Acetyloxy)-2-picolylamino]pentadecanoic acid: a potential radiotracer for evaluation of fatty acid metabolism
| Autor: | Jae Hak Lee, Yearn Seong Choe, Kyung-Han Lee, Byung-Tae Kim, Byung Chul Lee, Yong Choi, Donghyun Kim, Hyun Ju Sung, Dae Yoon Chi |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Male
Biomedical Engineering Uptake ratio Pharmaceutical Science Bioengineering Urine Pentadecanoic acid High-performance liquid chromatography chemistry.chemical_compound Mice Animals Tissue Distribution Tissue distribution Radioactive Tracers Pharmacology Mice Inbred ICR Chromatography Fatty acid metabolism Myocardium Organic Chemistry Fatty Acids Technetium chemistry Human plasma Yield (chemistry) Biotechnology |
| Zdroj: | Bioconjugate chemistry. 18(4) |
| ISSN: | 1043-1802 |
| Popis: | 99mTc(CO)3-15-[N-(Acetyloxy)-2-picolylamino]pentadecanoic acid (1a) was prepared by incorporating [99mTc(CO)3]+ into 15-[N-(hydroxycarbonylmethyl)-2-picolylamino]pentadecanoic acid (2a). The overall radiochemical yield of 1a after HPLC purification was 60-63%. Radiotracer 1a was found to be chemically stable when incubated in human plasma for 4 h at 37 degrees C. Tissue distribution studies showed that high radioactivity accumulated in the heart with rapid clearance. The maximum heart-to-blood uptake ratio was 1.87 at 5 min after a tail-vein injection. Radioactive metabolites were analyzed in urine samples of mice and corresponded to a 9.3:1 ratio of 99mTc(CO)3-5-[N-(acetyloxy)-2-picolylamino]pentanoic acid (1b) to 99mTc(CO)3-3-[N-(acetyloxy)-2-picolylamino]propionic acid (1c), indicating that 1a is mainly metabolized to 1b via beta-oxidation in the body. These results suggest that 1a is a promising radiotracer for evaluation of fatty acid metabolism in myocardium. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|