A new method of preventing restenosis is the use of a liquid-filled balloon containing a beta-emitting radionuclide. Rhenium-188 is one of the most common used radionuclides. In order to reduce the injury caused by high dose radioactivity in the event of balloon rupture, we have succeeded in preparing the 188Re-DTPA compound because DTPA can be excreted from kidney rapidly. The labeling methods and conditions were described. The yield of 188Re-DTPA was more than 90%. The biodistribution studies of 188Re-DTPA and 188Re perrhenate showed that radioactivity levels of 188Re perrhenate in the thyroid gland and stomach were higher than that of 188Re-DTPA, and the excretion of 188Re-DTPA was much faster than that of 188Re perrhenate. Data of the estimated absorbed doses of various tissues in rats using software of MIRDOSE showed the same results. The thyroid radiation values in the 188Re-DTPA group and 188Re perrhenate group were 0.041 and 0.563nGy / Bq, respectively. And the stomach radiation values were 0.043 and 0.118nGy / Bq, respectively. Our study therefore suggested that 188Re-DTPA was superior to 188Re perrhenale for use in endovascular brachytherapy.