Synthesis and Biological Evaluation of a New Type of 99mTechnetium-Labeled Fatty Acid for Myocardial Metabolism Imaging
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- 作者：Martin Walther ; Christian M. Jung ; Ralf Bergmann ; Jens Pietzsch ; Katrin Rode ; Karim Fahmy ; Peter Mirtschink ; Sebastian Stehr ; Anke Heintz ; Gerd Wunderlich ; Werner Kraus ; Hans-Juergen Pietzsch ; Joachim
- 刊名：Bioconjugate Chemistry
- 出版年：2007
- 出版时间：January 2007
- 年：2007
- 卷：18
- 期：1
- 页码：216 - 230
- 全文大小：465K
- 年卷期：v.18,no.1(January 2007)
- ISSN：1520-4812
文摘
Technetium-labeled fatty acids intended for myocardial metabolism imaging and the respective rhenium modelcomplexes were synthesized according to the "4 + 1" mixed-ligand approach and investigated in vitro and invivo. The non-radioactive rhenium model complexes were characterized by NMR, IR, and EA, and the geometricalimpact of the chelate unit on the integrity of the fatty acid head structure was determined by single-crystal X-rayanalyses. To estimate the diagnostic value of the 99mTc-labeled fatty acids, the compounds were investigated inexperiments in vitro and in biodistribution studies using male Wistar rats. The new fatty acid tracers contain themetal core in the oxidation states +3, well-wrapped in a trigonal-bipyramidal coordination moiety, which isattached at the 
-position of a fatty acid chain. This structural feature is considered to be a good imitation of thewell-established iodinated phenyl fatty acids. High heart extraction in perfused heart studies (up to 26% injecteddose (ID)) and noticeable heart uptake of the 99mTc tracers in vivo being in the order of 2% ID/g at 5 min(postinjection, pi.), accompanied by a good heart to blood ratio of 8, confirms that the new Tc compounds aresuitable as fatty acid tracers.
-position of a fatty acid chain. This structural feature is considered to be a good imitation of thewell-established iodinated phenyl fatty acids. High heart extraction in perfused heart studies (up to 26% injecteddose (ID)) and noticeable heart uptake of the 99mTc tracers in vivo being in the order of 2% ID/g at 5 min(postinjection, pi.), accompanied by a good heart to blood ratio of 8, confirms that the new Tc compounds aresuitable as fatty acid tracers.