新型~(99m)Tc标记肾显像剂的研究——Ⅰ.~(99m)Tc—MAG_3的合成和初步生物评价

THE STUDIES ON NEW ~(99m)Tc—LABELLED RENAL IMAGING AGENTS——Ⅰ. THE SYNTHESIS AND PRELIMINARY BIOLOGICAL EVALUATION OF ~(99m)Tc—MAG_3

摘要: 本文合成了三酰胺单巯基配体MAG_3(硫代乙酰基三甘氨肽),采用金属锡直接还原法,在pH>8.5,反应温度为95℃,反应时间>8min的条件下,MAG_3与~(99m)Tc络合,产额>98％。用纸层析法分析产物纯度,以丙酮和生理盐水两种展开剂作为展开体系,能够快速、有效地将还原水解Tc,~(99m)TcO_4与络合物分开。动物实验表明:~(99m)Tc-MAG_3显像质量优良、肾排泄快、是一种理想的取代~(131)I-OIH(邻碘马尿酸)的肾放射性药物。

Abstract: A new ligand for ~(99m)Tc based on triamide monomercaptide mercaptoacetyltriglycine (MAG_3) was synthesized. ~(99m)Tc-MAG_3 Was obtained by greater than 98% in basic medium (pH>8.5), reaction time>8 min at 95℃ and using solid tin as reducing agent. Ideal developing agents, a) Actone and b) physiological saline, were found for examining purity of the complex using paper chromatography. The preliminary animal results suggest that ~(99m)Tc-MAG_3 may be a satisfactory alternative to ~(131)I-OIH.