对氨基马尿酸类似物的合成及其99m锝标记

Synthesis of p-aminohippuric acid analog and its labeling by technetium-99m.

作者信息

Zmbova B, Djokić D, Bogdanova V, Tadzer I, Ajdinović B, Rastovac M

机构信息

Institute for Radioisotopes, Boris Kidric Institute of Nuclear Sciences, Vinca, Belgrade, Yugoslavia.

出版信息

Int J Rad Appl Instrum A. 1989;40(3):225-34. doi: 10.1016/0883-2889(89)90152-4.

DOI:10.1016/0883-2889(89)90152-4

PMID:2541109

Abstract

A procedure is described for the synthesis of p-[(bisacarboxymethyl)aminomethyl carbamino] hippuric acid (PAHIDA). The compound was identified by i.r. and NMR spectroscopy. A lyophilized complex was prepared and labeled with 99mTc. The purity of the preparation is better than 98%. The stability of the 99mTc-PAHIDA complex is achieved 8 h after labeling. Biodistribution tested on white rats shows a maximum accumulation in kidneys of 6-10% within 2 min after injection, while the accumulation in the liver is 2-4% of the administrated dose. Preliminary clinical studies of 99mTc-PAHIDA on patients and its comparison with 131I-hippuran showed that the 99Tc-PAHIDA preparation has excellent characteristics for visualization of kidneys. However, it has slightly slower urinary elimination compared to hippuran, which it makes possible to use PAHIDA as a replacement of hippuran to a certain extent.

摘要

描述了一种合成对-[(双羧甲基)氨甲基氨基甲酰基]马尿酸(PAHIDA)的方法。通过红外光谱和核磁共振光谱对该化合物进行了鉴定。制备了冻干复合物并用99mTc进行标记。制剂的纯度优于98%。99mTc-PAHIDA复合物在标记后8小时达到稳定状态。在白鼠身上进行的生物分布试验表明，注射后2分钟内肾脏中的最大蓄积量为6-10%，而肝脏中的蓄积量为给药剂量的2-4%。对患者进行的99mTc-PAHIDA初步临床研究及其与131I-马尿酸的比较表明，99mTc-PAHIDA制剂在肾脏显影方面具有优异的特性。然而，与马尿酸相比，其尿液清除速度略慢，这使得PAHIDA在一定程度上可以替代马尿酸。