원저 : 새로운 심근관류 영상 화합물로서 99mTc - Ethyl - 3 - Isocyanobutyrate의 합성 , 표지 및 체내동태에 대한 연구 ( Synthesis Characterization and Biodistribution of 99mTc - Ethyl - 3 - Isocyanobutyrate as a New Myocardial Perfusion Agent ) () |
Author |
이명철(Myung Chul Lee),조정혁(Jung Hyuck Cho),이동수(Dong Soo Lee),임상무(Sang Moo Lim),오승준(Seung Joon Oh),정수욱(Soo Wook Chung),이경한(Kyung Han Lee),정재민(Jae Min Jeong),정준기(June Key Chung),고창순(Chang Soon Koh), |
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Affiliation |
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Abstract |
Technetium labeled isonitrile analogues are widely used
as myocardial perfusion imaging agents. We synthesized
and characterized a new isonitrile compound, ethyl 3-
isocyanobutyrate (EIB). Proton and 13C NMR spectroscopy
and thin layer chromatography with a C18 coat was
performed. EIB was easily labeled with 99mTcO4-with
sodium dithionite. The labeling efficiency measured by
RP-HPLC was over 95%. The labeled product was stable
with dilution in normal saline and with prolonged
incubation at room temperature. There was no formation
of secondary products or free 99mTcO4. In vivo kinetics
study of Tc-99m(I) labeled EIB in rabbits showed
adequate myocardial uptake, good contrast against lung
background, and relatively rapid liver clearance. The
heart to lung ratio was over 2.5 and the heart to liver
ratio was approximately from 0.4 to 5 at 60 minutes
post injection. Hepatic clearance of Tc-99m-MIBI was
faster (t1/2,=6 minutes) than that of Tc-99m-MIBI. In
vivo kinetics observed in dog was similar to that in
rabbit but there was faster gallbladder filling, and
thus lower liver background. SPECT imaging of the
canine myocardium showed favorable imaging
characteristics. However, biodistribution in mice
demonstrated a myocardial % injected dose/organ of less
than 0.1%. This was thought to be due to interspecies
difference in plasma esterase activity. In human
plasma, Tc-99m(I) labeled EIB was stable for at least 2
hours, without production of secondary products by
HPLC. We conclude that ethyl 3-isocyanobutyrate may be
a potential new myocardial perfusion imaging agent and
deserves further investigation as to its usefulness for
clinical use. |
Keyword |
Myocardial SPECT, 99mTc-M1BI, Ethyl 3-isocyanobutyrate |
Full text Article |
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