新型~(99)Tc~m标记肾显像剂的研究 Ⅱ ~(99)Tc~m-MAG_2的合成及与~(99)Tc~m-MAG_3和~(99)Tc~(m~2)-DTPA的显像比较

STUDIES ON THE NEW ~(99)Tc~m-LABELLED RENAL IMAGING AGENTS Ⅱ. SYNTHESIS OF ~(99)Tc~m-MAG_2 AND IMAGING COMPARISON WITH ~(99)Tc~m-MAG_3 AND ~(99)Tc~n-DTPA

摘要: 合成了一种新型配体Bz-MAG 2(苯甲酰硫代乙酰基双甘氨肽),研究了该配体与~(99)Tc~m络合的影响因素(如反应体系pH值、反应温度和反应时间等),给出了络合产额≥98％的反应条件。在大白兔体内的显像结果表明:~(99)Tc~m-MAG_2的肾显像质量以及肾排泄速度都大大优于目前临床上常用的~(99)Tc~m肾显像剂~(99)Tc~m-DTPA(二乙撑三胺五乙酸),而稍次于~(99)Tc~m-MAG_3(巯基乙酰基三甘氨肽)。

Abstract: Changing the length of peptide chain, a new ligand,B_2-MAG_2 (benzoylthioacetyl diglycine), was synthesized. The effects of the pH value, reaction temperature and reaction time on the formation of ~(99)Tc~m-MAGa were studied and the preparation procedure with the complexing yield up to 98％ was established. The results on rabbits showed that both imaging quality and excretion rate of ~(99)Tc~m-MAG_2 were more superior to those of ~(99)Tc~m-DTPA (diethylenetriamine pentaacetate), which is currently used for renal imaging in clinic, while slightly inferior to ~(99)Tc~m-MAG_3 (mercaptoacetyl triglycine).