^(99)Tc^mN-DMCHI和^(99)Tc^m-DMCHI的制备及其生物分布

Synthesis and Biodistribution of ^(99)Tc^mN-DMCHI and ^(99)Tc^m-DMCHI

合成并表表征了新的异腈配体2,3 二甲基环己基异腈(DMCHI)及其铜络盐。分别通过配体交换法和直接标记法制备得到放化纯大于95%的脂溶性配合物99TcmN DMCHI和99Tcm DMCHI,二者在室温下均可稳定6h以上。在正常小鼠体内的生物分布实验结果表明,99TcmN DMCHI和99Tcm DMCHI在血液中均有较高的摄取和很好的滞留,而且血/心、血/肝和血/肺比值均大于1,有望用于心血池显像。

An isonitrile ligand 2,3-dimethyl cyclohexylisonitrile (DMCHI) and its copper salt (Cu(Ⅰ)(DMCHI)_4BF_4) are synthesized and characterized by IR,~1H NMR and elemental analysis.The complexes ^(99)Tc^mN-DMCHI and ^(99)Tc^m-DMCHI are prepared by ligand exchange reaction and directly labeling method,respectively.The results of partition coefficient and stability studies indicate that the complexes are lipophilic and stable over a period of 6 h at room temperature.Biodistribution of the new complexes in mice showe that these two complexes all have high blood uptake and retention in blood very well.The artios of blood-to-heart,blood-to-liver and blood-to -lugn at 5 min post-injection are 6.53,2.11 and 1.27 for ^(99)Tc^m-DMCHI and 5.29,1.79 and 1.18 for ^(99)Tc^mN-DMCHI,respectively.Based on these promising properties it is worthy to develop these ^(99)Tc^m labeled complexes as potential blood pool agents.