Abstract |
Achieving a (⁹⁹m)Tc-labeled fluoroquinolone derivative as a single photon emission computed tomography (SPECT) tracer is considered to be of great interest. The norfloxacin dithiocarbamate (NFXDTC) was synthesized and radiolabeled with a [(⁹⁹m)TcN]²(+) intermediate to form the (⁹⁹m)TcN-NFXDTC complex in high yield. The radiochemical purity of (⁹⁹m)TcN-NFXDTC was over 90%, as measured by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC), without any notable decomposition at room temperature over a period of 6 h. The partition coefficient and electrophoresis results indicated that (⁹⁹m)TcN-NFXDTC was lipophilic and neutral. The bacterial binding assay studies showed tht (⁹⁹m)TcN-NFXDTC had a good binding affinity. Biodistribution results in bacterial infected mice showed that (⁹⁹m)TcN-NFXDTC had a higher uptake at the sites of infection and better abscess/blood and abscess/muscle ratios than those of (⁹⁹m)Tc- ciprofloxacin and (⁹⁹m)TcN- CPFXDTC ( CPFXDTC = ciprofloxacin dithiocarbamate). The biodistribution results of (⁹⁹m)TcN-NFXDTC in bacterially infected mice and in mice with turpentine-induced abscesses indicated that (⁹⁹m)TcN-NFXDTC was suited to be a bacteria-specific infection imaging agent. Single photon emission computed tomography (SPECT) image studies showed there was a visible accumulation in infection sites, suggesting that it would be a promising candidate for bacterial infection imaging.
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Authors | Shijian Zhang, Weifang Zhang, Yue Wang, Zhonghui Jin, Xuebin Wang, Junbo Zhang, Yanyan Zhang |
Journal | Bioconjugate chemistry
(Bioconjug Chem)
Vol. 22
Issue 3
Pg. 369-75
(Mar 16 2011)
ISSN: 1520-4812 [Electronic] United States |
PMID | 21319731
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Ligands
- Organotechnetium Compounds
- norfloxacin dithiocarbamate
- Norfloxacin
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Topics |
- Animals
- Bacterial Infections
(diagnostic imaging)
- Drug Stability
- Electrophoresis, Paper
- Inflammation
(diagnostic imaging)
- Isotope Labeling
- Ligands
- Male
- Mice
- Norfloxacin
(analogs & derivatives, chemical synthesis, chemistry, pharmacokinetics)
- Organotechnetium Compounds
(chemistry)
- Rabbits
- Tomography, Emission-Computed, Single-Photon
(methods)
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