Synthesis and biodistribution of two novel 99mTc nitrido dithiocarbamate complexes containing heterocyclic linkage as potential brain perfusion imaging agents

摘要

In the present study, two novel 99mTc nitrido dithiocarbamate complexes containing heterocyclic linkage, the bis(N-2-(1-piperidyl)ethyl dithiocarbamato) nitrido technetium-99m complex 99mTcN(PPEDTC)2 and bis(N-2-(1-pyrrolidino)ethyl dithiocarbamato) nitrido technetium-99m complex 99mTcN(PREDTC)2 have been synthesized by the reduction of 99mTcO4 ? into [99mTcN]2+ with stannous chloride in the presence of succinic dihydrazide and propylenediamine tetraacetic acid, followed by the addition of the corresponding dithiocarbamate ligands. The radiochemical purity of the complexes were over 90% as measured by thin layer chromatography (TLC). In vitro studies showed that the complexes possessed good stability. Their partition coefficients indicated that they were lipophilic complexes. Biodistribution in mice showed that the 99mTcN(PPEDTC)2 complex accumulated in brain with high uptake and good retention. As compared with the 99mTcN(PREDTC)2 complex, the former showed much higher brain uptake than the latter.