Gianolli L, Dosio F, Matarrese M, Colombo F, Cutler C, Stepniak-Biniakiewicz D, Deutsch E, Savi A, Lucignani G, Fazio F
INB-CNR, University of Milan, Department of Nuclear Medicine, H San Raffaele, Italy.
Nucl Med Biol. 1996 Nov;23(8):927-33. doi: 10.1016/s0969-8051(96)00135-7.
We propose a renal imaging agent, the 99mTc complex of the bidentate-N,S chelate N-(mercaptoacetyl)glycine (99mTc-2GAM), with the imaging characteristics of 99mTc-DMSA but a faster kidney uptake; chemical evidence supports the formulation of 99mTc-2GAM as [Tc(v)(O)(GAM)2]-. After biodistribution and toxicity studies in animals, 99mTc-2GAM was evaluated in five normal volunteers. 99mTc-2GAM is rapidly cleared from the blood (t1/2 = 9 min) and 50% of the ID is excreted in the urine in the first 2 h. Dynamic data show a rapid renal uptake that increases up to 1 h with no significant wash-out between 1 and 8 h. The uptake in each kidney ranges from 11.3% to 20.7% ID. Low, stable liver uptake is observed. No significant activity is detected in other organs. We showed no differences between 99mTc-2GAM and 99mTc-DMSA compared in three patients with unilateral kidney disease. We conclude that 99mTc-2GAM has good practical and dosimetric features for renal imaging.
我们提出了一种肾脏显像剂，即双齿-N,S螯合物N-(巯基乙酰基)甘氨酸（99mTc-2GAM）的99mTc络合物，它具有99mTc-DMSA的显像特征，但肾脏摄取更快；化学证据支持将99mTc-2GAM制备为[Tc(v)(O)(GAM)2]-。在对动物进行生物分布和毒性研究后，对5名正常志愿者进行了99mTc-2GAM的评估。99mTc-2GAM从血液中迅速清除（t1/2 = 9分钟），给药量的50%在最初2小时内随尿液排出。动态数据显示肾脏摄取迅速，在1小时内不断增加，在1至8小时之间无明显洗脱。每个肾脏的摄取量占给药量的11.3%至20.7%。观察到肝脏摄取量低且稳定。在其他器官中未检测到明显活性。在3名单侧肾病患者中，我们发现99mTc-2GAM与99mTc-DMSA之间无差异。我们得出结论，99mTc-2GAM在肾脏显像方面具有良好的实用性和剂量学特征。
