99mTc(CO)3-AOPA colchicine conjugate as a potential tumor imaging agent
AbstractAbstract
[en] This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of the 99mTc(CO)3-AOPA colchicine conjugate. The novel ligand was successfully synthesized by conjugation of N-(acetyloxy)-2-picolylamino (AOPA) to deacetylcolchicine via a short carbonyl-methylene linker. Radiolabeling was performed in high yield with [99mTc(CO)3]+ core. 99mTc(CO)3-AOPA colchicine conjugate was hydrophilic and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that 99mTc(CO)3-AOPA colchicine conjugate accumulated in the tumor with good uptake and retention. However, its clearance from normal organs was not so fast, resulting in poor T/NT ratios. Further modification on the linker or/and 99mTc-chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress. (author)
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Journal Article
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Journal of Radioanalytical and Nuclear Chemistry; ISSN 0236-5731; ; CODEN JRNCDM; v. 288(2); p. 635-639
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ALKALOIDS, ANIMALS, ANTIMITOTIC DRUGS, ANTIPYRETICS, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, CENTRAL NERVOUS SYSTEM AGENTS, CENTRAL NERVOUS SYSTEM DEPRESSANTS, DISEASES, DRUGS, HOURS LIVING RADIOISOTOPES, INTERMEDIATE MASS NUCLEI, INTERNAL CONVERSION RADIOISOTOPES, ISOMERIC TRANSITION ISOTOPES, ISOTOPES, MAMMALS, NUCLEI, ODD-EVEN NUCLEI, ORGANIC COMPOUNDS, RADIOISOTOPES, RODENTS, TECHNETIUM ISOTOPES, VERTEBRATES, YEARS LIVING RADIOISOTOPES
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