99mTc(CO)3–AOPA colchicine conjugate as a potential tumor imaging agent
| Autor: | Tingting Niu, Xiaojiang Duan, Huining Mao, Jing Yang, Jianjun Wang |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Tumor imaging
Deacetylcolchicine Biodistribution Chemistry Stereochemistry Health Toxicology and Mutagenesis Public Health Environmental and Occupational Health Ligand (biochemistry) Pollution Analytical Chemistry chemistry.chemical_compound Nuclear Energy and Engineering In vivo Biophysics Colchicine Radiology Nuclear Medicine and imaging Linker Spectroscopy Conjugate |
| Zdroj: | Journal of Radioanalytical and Nuclear Chemistry. 288:635-639 |
| ISSN: | 1588-2780 0236-5731 |
| DOI: | 10.1007/s10967-011-0983-4 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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