Synthesis and biological evaluation of a novel (99m)Tc nitrido radiopharmaceutical with deoxyglucose dithiocarbamate, showing tumor uptake.
The deoxyglucose dithiocarbamate (DGDTC) was synthesized and radiolabelled with [(99m)TcN](2+) intermediate to form the (99m)TcN-DGDTC complex. The radiochemical purity of the (99m)TcN-DGDTC complex was over 90%, as measured by TLC and by HPLC, without any notable decomposition at room temperature over a period of 6h. The partition coefficient and electrophoresis results indicated that this complex was hydrophilic and neutral. The biodistribution of (99m)TcN-DGDTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time and reached 2.32 and 1.68 at 4h post-injection, suggesting it would be a promising candidate for tumor imaging.
Beijing Normal University, Ministry of Education, PR China. zhjunbo@bnu.edu.cn
Junbo
J
Zhang
Jialei
J
Ren
Xiao
X
Lin
Xuebin
X
Wang
D000818:Animals; D002219:Carbamates / Q000138:chemical synthesis / Q000737:chemistry; D003847:Deoxyglucose / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry; D007553:Isotope Labeling; D051379:Mice; D009369:Neoplasms / Q000000981:diagnostic imaging*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D014018:Tissue Distribution
D002219:Carbamates; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C541546:deoxyglucose dithiocarbamate; D003847:Deoxyglucose