Filters
Results 1 - 1 of 1
Results 1 - 1 of 1.
Search took: 0.025 seconds
AbstractAbstract
[en] This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of 99mTc(CO)3-labeled pegylated (PEG) 2-nitroimidazoles for tumor hypoxia imaging. The novel 2-nitroimidazole derivatives were successfully synthesized by conjugation of tridendate chelators to 2-nitroimidazole via PEG3 linker. Radiolabeling was performed in high yield with [99mTc(CO)3]+ core to get cationic [99mTc(CO)3(BPA-PEG3-NIM)]+, neutral [99mTc(CO)3(AOPA-PEG3-NIM)] and anionic [99mTc(CO)3(IDA-PEG3-NIM)]- respectively, all of which were hydrophilic and stable at room temperature. Biodistribution studies in tumor-bearing mice showed that 99mTc(CO)3-labeled pegylated 2-nitroimidazoles accumulated in the tumor with low uptake. 99mTc-chelate and charge had significant impact on partition coefficient, radiotracer tumor uptake and pharmacokinetic properties. The results indicate the need for synthetic modification of the parent 2-nitroimidazole derivatives and the 99mTc-chelate with a view to improve the tumor targeting efficacy and in vivo kinetic profiles. (author)
Primary Subject
Source
47 refs.
Record Type
Journal Article
Journal
Journal of Radioanalytical and Nuclear Chemistry; ISSN 0236-5731; ; CODEN JRNCDM; v. 300(3); p. 1013-1020
Country of publication
ALCOHOLS, ANIMALS, ANTINEOPLASTIC DRUGS, AZOLES, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, BIOMEDICAL RADIOGRAPHY, DIAGNOSTIC TECHNIQUES, DISEASES, DISTRIBUTION, DRUGS, GLYCOLS, HETEROCYCLIC COMPOUNDS, HOURS LIVING RADIOISOTOPES, HYDROXY COMPOUNDS, IMIDAZOLES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, LABELLED COMPOUNDS, MAMMALS, MATERIALS, MEDICINE, MICE, NITRO COMPOUNDS, NUCLEAR MEDICINE, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, ORGANIC NITROGEN COMPOUNDS, ORGANIC POLYMERS, POLYMERS, RADIOACTIVE MATERIALS, RADIOISOTOPES, RADIOLOGY, RADIOSENSITIZERS, RESPONSE MODIFYING FACTORS, RODENTS, TECHNETIUM ISOTOPES, TRANSGENIC ANIMALS, VERTEBRATES, YEARS LIVING RADIOISOTOPES
Reference NumberReference Number
INIS VolumeINIS Volume
INIS IssueINIS Issue