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KMID : 0363819930270020223
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Korean Journal of Nuclear Medicine
1993 Volume.27 No. 2 p.223 ~ p.232
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Synthesis Characterization and Biodistribution of 99mTc-Ethy1-3-Isocyanobutyrate as a New Myocardial Perfusion Agent
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이명철
조정혁/이동수/임상무/오승준/정수욱/이경한/정재민/정준기
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Abstract
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Technetium labeled isonitrile analogues are widely used as myocardial perfusion imaging agents.
We synthesized and characterized a new isonitrile compound, ethyl 3-isocyanobutyate (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 99mTc (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 99mTc-MI?BI was faster (t1/2=6 minutes) than that of 99mTc-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, 99mTc(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.
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KEYWORD
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