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Preparation of (186Re)Re-DMSA and its bio-distribution studies.

机译:(186Re)Re-DMSA的制备及其生物分布研究。

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摘要

99mTc(V)-DMSA is widely used for imaging medullary carcinoma and hence 186/188Re(V)-DMSA is suggested as a potential agent for treating medullary carcinoma. In the present paper, we report the work carried out for the preparation of [186Re]Re(V)-DMSA and it's bio-distribution studies in Wistar rats. The complex was prepared by reducing 186Re (100 micrograms, 0.54 microM, approximately 150 MBq) in the presence of DMSA (2 mg, 11 microM) with stannous chloride (0.4 mg, 2.2 microM) in acidic medium at pH 2. The reaction was taken to completion by heating the complex in a boiling water bath for 30 min. Bio-distribution studies carried out revealed that pharmacological behaviour of 186Re(V)-DMSA is similar to that of 99mTc(V)-DMSA except that the kidney uptake is marginally higher. The kidney uptake reduced significantly when the pH of the complex was adjusted to 8 prior to injection. The in vitro stability studies of this complex suggest that the product formed is stable and could be used for clinical trials.
机译:99mTc(V)-DMSA被广泛用于髓样癌的成像,因此186 / 188Re(V)-DMSA被认为是治疗髓样癌的潜在药物。在本文中,我们报告了[186Re] Re(V)-DMSA的制备及其在Wistar大鼠体内的生物分布研究。通过在DMSA(2 mg,11 microM)存在下,在pH 2的酸性介质中用氯化亚锡(0.4 mg,2.2 microM)还原186Re(100 mg,0.54 microM,大约150 MBq)来制备复合物。通过在沸水浴中加热复合物30分钟来完成。进行的生物分布研究表明,186Re(V)-DMSA的药理行为与99mTc(V)-DMSA的药理行为相似,只是肾脏摄取略高。当注射前将复合物的pH值调节至8时,肾脏的肾脏吸收显着降低。该复合物的体外稳定性研究表明所形成的产物是稳定的,可用于临床试验。

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