Technetium-99m-labeled-5-{2-sulfanylethyl-[2-(2-sulfanylethylamino)acetyl]amino}-methyl-2′-deoxy- uridine (99mTc-ANMdU) was reported. The precursor ANMdU was synthesized by six-step reactions and all intermediates were verified with MS and 1HNMR. Using SnCl2 as reducing agent, a labeling reaction was carried out at 100°C for 30 min. The radiochemical purity of the 99mTc-ANMdU was 96.68%. Partition coefficients were 0.92 and 0.70 at pH 7.0 and 7.4 of the phosphate buffer saline, respectively. Biodistribution of 99mTc-ANMdU in normal mice showed that the initial uptake of 99mTc-ANMdU in vivo and the clearance was rapid.
LU ChunxiongJIANG QuanfuYU HuixinWANG SongpeiLi XiaominWANG Zhengwu
The synthesis and labeling of ^(99m)Tc-N^3-(N'-[2-sulfanyl-ethylamino)acetyl]-2-aminoethyl-sulfanyl-1-hexanamide}thymidine (^(99m)Tc-NHT) were studied.In the presence of sodium glucoheptonate(GH) and ethylene diamine tetraacetic acid(EDTA),^(99m)Tc-NHT was obtained by using bisaminoethanethiol(N_2S_2) as a bifunctional coupling agent.The radiochemical purity of the ^(99m)Tc-NHT was over 95%.Biodistribution of ^(99m)Tc-NHT was performed in hepatoma HepA tumor-bearing mice.At 2 h p.i.,the ratios of tumor-to-muscle,tumor-to-bone and tumor-to-blood were 4.41±0.32,2.45±0.24 and 1.51±0.18,respectively.
Chun Xiong LuZheng Wu WangQuan Fu JiangJie TangCheng TanJian Kang-Zhang
