99mTc(CO)3-15-[N-(Acetyloxy)-2-picolylamino]pentadecanoic acid: a potential radiotracer for evaluation of fatty acid metabolism.
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.
Lee
Byung Chul
BC
Department of Chemistry, Inha University, 253 Yonghyundong, Namgu, Inchon 402-751, Korea.
Kim
Dong Hyun
DH
Lee
Jae Hak
JH
Sung
Hyun Ju
HJ
Choe
Yearn Seong
YS
Chi
Dae Yoon
DY
Lee
Kyung-Han
KH
Choi
Yong
Y
Kim
Byung-Tae
BT
D000818:Animals; D005227:Fatty Acids / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000652:urine; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009206:Myocardium / Q000378:metabolism; D011849:Radioactive Tracers; D013667:Technetium / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000652:urine; D014018:Tissue Distribution
D005227:Fatty Acids; D011849:Radioactive Tracers; D013667:Technetium; C117025:pentadecanoic acid