Synthesis and biodistribution of a novel (99m)TcN complex of ciprofloxacin dithiocarbamate as a potential agent for infection imaging.
The ciprofloxacin dithiocarbamate (CPFXDTC) was synthesized and radiolabeled with [(99m)TcN](2+) intermediate to form the (99m)TcN-CPFXDTC complex in high yield (>95%). No decomposition of the complex at room temperature was observed over a period of 6 h. Its partition coefficient indicated that it was a good lipophilic complex. The bacterial binding assay studies showed (99m)TcN-CPFXDTC had a better binding affinity as compared with (99m)Tc-ciprofloxacin. Biodistribution results in induced infection mice showed (99m)TcN-CPFXDTC had higher uptake at the sites of infection and better abscess/blood ratio than that of (99m)Tc-ciprofloxacin, suggesting (99m)TcN-CPFXDTC would be a novel potential infection imaging agent.
Zhang
Junbo
J
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China. zhjunbo@bnu.edu.cn
Guo
Haixun
H
Zhang
Shijian
S
Lin
Yan
Y
Wang
Xuebin
X
D000818:Animals; D002939:Ciprofloxacin / Q000031:analogs & derivatives / Q000097:blood / Q000138:chemical synthesis / Q000493:pharmacokinetics; D003952:Diagnostic Imaging; D008297:Male; D051379:Mice; D015394:Molecular Structure; D015609:Organotechnetium Compounds / Q000097:blood / Q000138:chemical synthesis / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals; D013859:Thiocarbamates / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014915:Whole-Body Counting
C532389:99mTc-CPFXDTC; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D013859:Thiocarbamates; C532390:ciprofloxacin dithiocarbamate; D002939:Ciprofloxacin