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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N2 S2 或N3S型小分子多肽新配体 ,并通过了IR ,1HNMR ,13CNMR ,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99Tcm 标记 ,研究了配合物在小鼠体内的生物分布特征。结果表明 ,99Tcm 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 ;99Tcm 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 ;99Tcm MVTC和99Tcm MPTC心肌初始摄取均较高 ,但在心肌和血中的清除速度较快
Based on the structure-activity relationship, we introduced four suitable natural amino acids with MAG3 as the basic molecular framework, and designed and synthesized four new ligands of N2 S2 or N3S small molecule peptides. Their structures were confirmed by IR, 1HNMR, 13CNMR and MS spectra Elemental analysis characterization. The four ligands were labeled with 99Tcm by using calcium glucoheptonate (GH) exchange method. The biodistribution of the complexes in mice was studied. The results showed that 99Tcm MVGG had higher renal uptake, longer residence time, faster serum clearance and higher activity ratio of kidney to other tissues, Renal / blood) activity ratio, but the renal clearance was faster and the ratio of R (kidney / liver) activity was lower. The initial uptake of 99Tcm MVTC and 99Tcm MPTC was higher, but the clearance rate in myocardium and blood was faster