新型~(99)Tc~m标记肾显像剂的研究——Ⅲ.~(99)Tc~m-MAG_2的结构测定

STUDIES ON THE NEW ~(99)Tc~m-LABELLED RENAL IMAGING AGENTS Ⅲ.INVESTIGATION OF THE STRUCTURE OF ~(99)Tc~m-MAG_2

  • 摘要: 在合成出~(99)Tc~m-MAG_2(巯基乙酰基双甘氨肽)的基础上,本文采用萃取、阴离子交换和同位素示踪等分析方法,通过测定中心离子~(99)Tc~m的价态、~(99)Tc~m-MAG_2配位化合物表观电荷及其化学计量组成,研究了~(99)Tc~m-MAG_2的结构。结果表明:配位化合物中,~(99)Tc~m以+5价存在;在本实验条件下,配体中氧原子参与成键,~(99)Tc~m与MAG_2络合,形成结构与~(99)Tc~m-MAG_3(巯基乙酰基三甘氨肽)和~(99)Tc~m-DADS(N,N’-双(巯基乙酰基)乙撑二胺)类似的配位化合物Tc(V)ON_2SO。

     

    Abstract: ~(99)Tc~m-MAG_3(mercaptoacetyltriglycine), a recently developed renal imaging agent as an alternative to ~(131)I-OIH(hippuran), has been in use in clinic. In the study of ~(99)Tc~m-labelled renal radiopharmaceuticals, an important direction is the investigation of the relationship between their structure and behavior in vivo through changing the structure of ligands, which combine with ~(99)Tc~m to form the ~(99)Tc~m-complexes. To reveal the reasons that lead to the differences between ~(99)Tc~m-MAG_2 (mercap toacetyl diglycine), a potential renal imaging agent synthesized lately in our laboratory, ~(99)Tc~m-MAG_3 as well as ~(99)Tc~m DADS (N,N'-bis (mercaptoacetamido) ethylene diamine), the structure of ~(99)Tc~mMAG_2 is comfirmed by determining the oxidation state of ~(99)Tc~m, apparent charge and stoichiometric composition of the complex. The results show that ~(99)Tc~m complexes with MAG_2 to form Tc (Ⅴ) ON_2SO, which is similar to ~(99)Tc~m-MAG_3 and ~(99)Tc~m-DADS, with stoichiometric composition 1: 1, and that the oxidation state of ~(99)Tc~m is five and carboxylate oxygen is the donor atom.

     

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