Details

Autor(en) / Beteiligte

• Lee, Byung Chul
• Kim, Dong Hyun
• Lee, Jae Hak
• Sung, Hyun Ju
• Choe, Yearn Seong
• Chi, Dae Yoon
• Lee, Kyung-Han
• Choi, Yong
• Kim, Byung-Tae

Titel

99mTc(CO)3-15-[N-(Acetyloxy)-2-picolylamino]pentadecanoic Acid:  A Potential Radiotracer for Evaluation of Fatty Acid Metabolism

Ist Teil von

• Bioconjugate chemistry, 2007-07, Vol.18 (4), p.1332-1337

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2007

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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 °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 β-oxidation in the body. These results suggest that 1a is a promising radiotracer for evaluation of fatty acid metabolism in myocardium.