Document Detail


16-Cyclopentadienyl tricarbonyl 99mTc 16-oxo-hexadecanoic acid: synthesis and evaluation of fatty acid metabolism in mouse myocardium.
MedLine Citation:
PMID:  18503263     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
We synthesized 16-cyclopentadienyl tricarbonyl 99mTc 16-oxo-hexadecanoic acid (99mTc-CpTT-16-oxo-HDA, 1) and investigated its potential as a radiotracer for evaluating fatty acid metabolism in myocardium. Radiotracer 1 was synthesized in 22.6 +/- 6.3% decay-corrected yield by a double ligand transfer reaction between the ferrocene adduct of methyl hexadecanoate ( 2) and Na99mTcO 4 in the presence of Cr(CO)6 and CrCl3, followed by hydrolysis of the methyl ester group. Radiotracer 1 was found to be chemically stable (99% at 6 h) when incubated in human serum. A tissue distribution study in mice showed that high radioactivity accumulated in heart (9.03%ID/g at 1 min and 5.41%ID/g at 5 min postinjection) with rapid clearance and that heart to blood uptake ratios increased with time (2.13 at 5 min and 3.76 at 30 min postinjection). Metabolite analysis of the heart tissues using a simple extraction method showed that 99mTc-CpTT-4-oxo-butyric acid was detected as the major radioactive metabolite by HPLC, suggesting that 1 is metabolized to 99mTc-CpTT-4-oxo-butyric acid via beta-oxidation in myocardium.
Authors:
Byung Chul Lee; Dong Hyun Kim; Iljung Lee; Yearn Seong Choe; Dae Yoon Chi; Kyung-Han Lee; Yong Choi; Byung-Tae Kim
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-05-27
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  51     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2008 Jun 
Date Detail:
Created Date:  2008-06-19     Completed Date:  2008-09-05     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  3630-4     Citation Subset:  IM    
Affiliation:
Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, 50 Ilwon-dong, Kangnam-ku, Seoul 135-710, Korea.
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MeSH Terms
Descriptor/Qualifier:
Animals
Fatty Acids / metabolism*
Heart / radionuclide imaging
Humans
Male
Mice
Mice, Inbred ICR
Myocardium / metabolism*
Organotechnetium Compounds / chemical synthesis*,  chemistry,  pharmacokinetics
Radiopharmaceuticals / chemical synthesis*,  chemistry,  pharmacokinetics
Tissue Distribution
Chemical
Reg. No./Substance:
0/Fatty Acids; 0/Organotechnetium Compounds; 0/Radiopharmaceuticals; 0/technetium 99m 16-cyclopentadienyl tricarbonyl 16-oxohexadecanoic acid

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