Document Detail


Evaluation of D-isomers of O-18F-fluoromethyl, O-18F-fluoroethyl and O-18F-fluoropropyl tyrosine as tumour imaging agents in mice.
MedLine Citation:
PMID:  16699766     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The aim of this study was to evaluate the properties of the D-amino acid isomers O-(18)F-fluoromethyl tyrosine ((18)F-FMT), O-(18)F-fluoroethyl tyrosine ((18)F-FET) and O-(18)F-fluoropropyl tyrosine ((18)F-FPT) as tumour-detecting agents with PET in comparison with the corresponding L-isomers. L- or D-(18)F-FMT, (18)F-FET or (18)F-FPT, prepared by (18)F-fluoromethylation, (18)F-fluoroethylation or (18)F-fluoropropylation of L- and D-tyrosine, was intravenously injected into BALB/cA Jcl-nu mice bearing HeLa tumour cells. At 5, 15, 30 and 60 min post intravenous administration, the uptake of each compound in normal abdominal organs and xenotransplanted HeLa cells was determined using the tissue dissection method. Metabolic stability analyses of these compounds in the plasma were performed with the thin-layer chromatography method. In the plasma fraction, although L- and D-isomers of (18)F-FMT, (18)F-FET and (18)F-FPT provided comparable metabolic stability, D-isomers of these labelled compounds revealed a faster elimination rate than their L-isomers, with a higher peak uptake in the blood and kidney 5 min post administration. Compared with natural amino acid ligands, such as L-(11)C-methionine, the uptake of L-isomers of these labelled compounds was relatively low and stable in the abdominal organs, while D-isomers revealed much lower and faster clearance rates compared with the corresponding L-isomers. Among the abdominal organs, the pancreas showed relatively high uptake of all the labelled compounds used here, and the uptake of D-isomers was much lower than that of the L-isomers. Although tumour uptake levels of D-isomers of (18)F-FMT, (18)F-FET and (18)F-FPT were almost 95%, 43% and 39% of the uptake levels of each of the L-isomers 60 min post administration, the tumour-to-blood ratios of these D-isomers were 181%, 137% and 101% of the ratios of the corresponding L-isomers. D-isomers of (18)F-FMT and (18)F-FET indicated improved tumour-to-liver ratios compared with the corresponding L-isomers, and D-(18)F-FPT showed the highest tumour-to-pancreas ratio among all the other compounds assayed here. These results suggest that D-isomers of (18)F-fluoroalkyl tyrosine analogues are potential tracers for tumour imaging with PET.
Authors:
Hideo Tsukada; Kengo Sato; Dai Fukumoto; Takeharu Kakiuchi
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2006-05-13
Journal Detail:
Title:  European journal of nuclear medicine and molecular imaging     Volume:  33     ISSN:  1619-7070     ISO Abbreviation:  Eur. J. Nucl. Med. Mol. Imaging     Publication Date:  2006 Sep 
Date Detail:
Created Date:  2006-08-14     Completed Date:  2007-04-18     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101140988     Medline TA:  Eur J Nucl Med Mol Imaging     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  1017-24     Citation Subset:  IM    
Affiliation:
PET Center, Central Research Laboratory, Hamamatsu Photonics K.K., 5000 Hirakuchi Hamamatsu, Shizuoka, 434-8601, Japan. tsukada@crl.hpk.co.jp
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MeSH Terms
Descriptor/Qualifier:
Animals
Drug Evaluation, Preclinical
Female
Fluorine Radioisotopes / diagnostic use,  pharmacokinetics
Hela Cells
Humans
Mice
Mice, Inbred BALB C
Mice, Nude
Neoplasms, Experimental / metabolism,  radionuclide imaging*
Positron-Emission Tomography
Radiopharmaceuticals / chemistry,  diagnostic use*,  pharmacokinetics
Stereoisomerism
Tissue Distribution
Tyrosine / analogs & derivatives*,  chemistry,  diagnostic use,  pharmacokinetics
Chemical
Reg. No./Substance:
0/Fluorine Radioisotopes; 0/O-(18F)fluoromethyl-L-tyrosine; 0/O-(2-fluoroethyl)tyrosine; 0/O-(3-fluoropropyl)tyrosine; 0/Radiopharmaceuticals; 55520-40-6/Tyrosine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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