Comparison of a new Tc-99m renal function agent, Tc-99m mercaptoacetyltriglycine, with I-131 OIH
Comparison of a new Tc-99m renal function agent, Tc-99m mercaptoacetyltriglycine, with I-131 OIH
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新型 Tc-99m 肾功能药物 Tc-99m 巯基乙酰三甘氨酸与 I-131 OIH 的比较
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发表时间：
1985
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通讯作者：
A. Taylor
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作者：
D. Eshima;A. Fritzberg;S. Kasina;D. Johnson;A. Taylor
寻找Tc-99 m替代I-131马尿酸盐（OIH）的方法导致合成了（巯基乙酰基三甘氨酸）Tc-99 m MAG/sub 3/，这是一种具有单一立体化学形式的N/sub 3/S衍生物，适用于其制剂。对照组和丙磺舒给药组动物的小鼠生物分布研究表明，两组动物中Tc-99 m MAG/sub 3/的肾排泄均上级OIH。在大鼠中进行了蛋白结合研究、恒定输注清除率研究和提取效率，以确定该药物用于评价肾功能的潜力。在大鼠血浆中，TC-99 m MAG/sub 3/的蛋白结合率为78%，而OIH的蛋白结合率为34%。Tc-99 m MAG/sub 3/和OIH的恒定输注清除率值分别为2.70和2.11 ml/min/ 100 gm体重。在IV给予竞争性抑制剂丙磺舒和对氨基马尿酸（PAH）存在下测定清除率值。通过Tc-99 m MAG/sub 3/和OIH的动静脉差异在大鼠中进行了浸提效率研究。发现Tc-99 m MAG/sub 3/的萃取效率为84.8%，而OIH的萃取效率为69.4%。总之，在正常啮齿动物中，TC-99 m MAG/sub 3/比OIH清除更快，具有高特异性。在存在肾小管转运抑制剂的情况下，其清除率与经GFR校正的OIH更相似。«少
The search for a Tc-99m replacement for I-131 hippurate (OIH) has led to the synthesis of (mercaptoacetyltriglycine) Tc-99m MAG/sub 3/, a N/sub 3/S derivative with a single stereochemical form, amenable to it formulation. Mouse biodistribution studies in control and probenecid treated animals indicated that renal excretion of Tc-99m MAG/sub 3/ was superior to OIH in both groups of animals. Protein binding studies, constant infusion clearance studies and extraction efficiencies were performed in rats to determine the potential of this agent for evaluation of renal function. In rat plasma TC-99m MAG/sub 3/ was 78% protein bound while OIH was 34% bound. The constant infusion clearance values for Tc-99m MAG/sub 3/ and OIH were 2.70 and 2.11 ml/min/ 100 gm body weight respectively. Clearance values were determined in the presence of IV administered competitive inhibitors, probenecid and para-aminohippuric acid (PAH). Extraction efficiency studies were performed in rats by arterio-venous differences for Tc-99m MAG/sub 3/ and OIH. Tc-99m MAG/sub 3/ was found to have an extraction efficiency of 84.8% while 69.4% was found for OIH. In summary, TC-99m MAG/sub 3/ is cleared more rapidly than OIH in normal rodents with high specificity. Its clearance, in the presence of tubular transport inhibitors, was similarmore » to OIH when corrected for GFR.« less