Document Detail

Preliminary studies of 99mTc-BnAO and its analogues: synthesis, radiolabeling and in vitro cell uptake.
MedLine Citation:
PMID:  20152710     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: (99m)Tc-BnAO is one of the nonnitroimidazole hypoxia markers with the highest citation and could be potentially useful in both oncology and other clinical applications. However, it appears inferior in vitro due to lower absolute accumulation and smaller anoxic/normoxic uptake ratio. It is possible that the analogues of (99m)Tc-BnAO have higher hypoxia selectivity after the ligand of (99m)Tc-BnAO is modified. METHODS: 2,2'-(1,4-Diaminobutane)bis(2-methyl-3-butanone) dioxime (BnAO or HL91) and three novel analogues were synthesized and radiolabeled with technetium-99m. The cellular uptake of the radiolabeled complexes was determined in murine sarcoma S180 cell lines under anoxic and normoxic conditions. RESULTS: (99m)Tc-BnAO and its three novel analogues continuously accumulated in anoxic cells but not in normoxic ones, while the analogues showed earlier hypoxia selectivity and greater anoxic/normoxic differential. CONCLUSIONS: The analogues are superior to (99m)Tc-BnAO in terms of in vitro hypoxia selectivity and are viable candidates for further development as new nonnitroimidazole hypoxia markers in the future.
Xin Sun; Taiwei Chu; Xiangyun Wang
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-11-03
Journal Detail:
Title:  Nuclear medicine and biology     Volume:  37     ISSN:  1872-9614     ISO Abbreviation:  Nucl. Med. Biol.     Publication Date:  2010 Feb 
Date Detail:
Created Date:  2010-02-15     Completed Date:  2010-05-20     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9304420     Medline TA:  Nucl Med Biol     Country:  England    
Other Details:
Languages:  eng     Pagination:  117-23     Citation Subset:  IM    
Copyright Information:
(c) 2010 Elsevier Inc. All rights reserved.
Beijing National Laboratory for Molecular Sciences (BNLMS), Department of Applied Chemistry, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
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MeSH Terms
Biological Transport
Cell Hypoxia
Cell Line, Tumor
Cells / metabolism*
Chromatography, Thin Layer
Isotope Labeling
Magnetic Resonance Spectroscopy
Organotechnetium Compounds / chemical synthesis*,  chemistry,  metabolism*
Oximes / chemical synthesis*,  chemistry,  metabolism*
Sarcoma / metabolism,  pathology
Spectrometry, Mass, Electrospray Ionization
Technetium / chemistry*
Transition Temperature
Reg. No./Substance:
0/Organotechnetium Compounds; 0/Oximes; 0/technetium Tc 99m 4,9-diaza-3,3,10,10-tetramethyldodecan-2,11-dione dioxime; 7440-26-8/Technetium

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