Müller-Suur R, Müller-Suur C
Eur J Nucl Med. 1986;12(9):438-42. doi: 10.1007/BF00254747.
We investigated the renal clearance, the extrarenal clearance, the biodistribution, the plasma extraction ratio and the imaging quality on a scintillation camera of a new substance: 99mTc-mercaptoacetyltriglycine (MAG-3) in rats. Simultaneously 125I-hippurate (OIH) and 51Cr-EDTA were used as reference substances. In scintillation camera studies, 123I-hippurate served as reference. MAG-3 was prepared by kit labelling without further purification, as it would be used in clinical studies. However in three separate rats, HPLC purified MAG-3 was used. High renal clearance and extraction ratio was found but these were less than that for OIH (1.95 ml/min per 100 g BW vs 2.76 ml/min per 100 g BW and 64% vs 85% respectively). The extrarenal clearance was higher for MAG-3 than for OIH (0.20 ml/min per 100 g BW vs 0.04 ml/min per 100 g BW), presumably because of bile excretion. HPLC purification increased the renal excretion of MAG-3: the clearance was 2.53 ml/min per 100 g BW, the extraction fraction 75%, but the extrarenal clearance was unchanged. The imaging quality was comparable to that of 123I-hippurate in early pictures, but extrarenal activity, presumably representing bile, was observed in late pictures. We conclude that MAG-3 has some potential for the replacement of OIH but clinical studies are necessary to test whether the same conditions and limitations exist in humans.
99m锝-巯基乙酰三甘氨酸(MAG-3)的肾清除率、肾外清除率、生物分布、血浆提取率以及在闪烁相机上的成像质量。同时使用125I-马尿酸盐(OIH)和51Cr-乙二胺四乙酸作为参考物质。在闪烁相机研究中,123I-马尿酸盐用作参考。MAG-3是通过试剂盒标记制备的,未进一步纯化,因为它将用于临床研究。然而,在三只单独的大鼠中,使用了经高效液相色谱(HPLC)纯化的MAG-3。发现MAG-3具有较高的肾清除率和提取率,但低于OIH(分别为每100克体重1.95毫升/分钟 vs 每100克体重2.76毫升/分钟以及64% vs 85%)。MAG-3的肾外清除率高于OIH(每100克体重0.20毫升/分钟 vs 每100克体重0.04毫升/分钟),推测是由于胆汁排泄。HPLC纯化增加了MAG-3的肾排泄:清除率为每100克体重2.53毫升/分钟,提取分数为75%,但肾外清除率未改变。早期图像中MAG-3的成像质量与123I-马尿酸盐相当,但晚期图像中观察到肾外活性,推测代表胆汁。我们得出结论,MAG-3有取代OIH的一些潜力,但需要进行临床研究以测试在人类中是否存在相同的情况和局限性。