N_2S_2或N_3S型配体的合成、~(99)Tc~m标记及生物分布研究

以MAG3为基本分子骨架，根据构效关系，分别引入合适的天然氨基酸，设计合成了4种N2S2或N3S型小分子多肽新配体，并通过了IR，^1H NMR,^13C NMR,MS谱学鉴定和元素分析表征。采用葡庚糖酸钙（GH）交换法对4个配体进行了^99Tc^m标记，研究了配合物在小鼠体内的生物分布特征。结果表明，^99Tc^m-MVGG肾摄取较高，滞留时间较长，血清除快，且肾与其它组织的活度比值高，具备成为肾功能显像剂的条件；^99Tc^m-MPGG肾初始摄取较高，R（肾／血）活度比值高，但肾清除较快，R（肾／肝）活度比值较低；^99Tc^m-MVTC和^99Tc^m－MPTC心肌初始摄取均较高，但在心肌和血中的清除速度较快。

SYNTHESIS OF LABELED PEPTIDE COMPLEXES WITH TECHNETIUM-99m AND BIODISTRIBUTION IN MICE

Four new N 2S 2 or N 3S small peptide chelators are synthesized based on renal function imaging agent 99Tc m-MAG 3 as fundamental structure by introducing natural amino acids according to reasonable structure-activity relationships. All the new compounds are identified on the basis of the spectroscopic data, such as IR, 1H NMR, 13C NMR, MS and elemental analysis. All the chelators are labeled with technetium-99m and further tested for the biological activity in mice. The biodistribution results in mice indicate that 99Tc m-MVGG has high kidney uptake, good retention, quick blood clearance and high activity ratios of kidney to other tissues, suggesting that it would be a new potential renal function imaging agent; 99Tc m-MPGG has better kidney accumulation and higher activity ratios of kidney to blood; 99Tc m-MVTC and 99Tc m-MPTC have higher heart accumulation.