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[(186/188)铼]铼-乙二胺四乙酸(Re-Ec):制备及在血管内近距离放射治疗中可能应用的评估

[(186/188)Re] rhenium-ethylene dicysteine (Re-Ec): preparation and evaluation for possible use in endovascular brachytherapy.

作者信息

Das T, Banerjee S, Samuel G, Kothari K, Unni P R, Sarma H D, Ramamoorthy N, Pillai M R

机构信息

Radiopharmaceuticals Division Bhabha Atomic Research Centre, Mumbai, India.

出版信息

Nucl Med Biol. 2000 Feb;27(2):189-97. doi: 10.1016/s0969-8051(99)00097-9.

Abstract

188ReO(4)(-), (188)Re-MAG(3), and (188)Re-DTPA are currently under investigation as radiation sources in liquid-filled balloons for prevention of restenosis following coronary angioplasty. Because (99m)Tc-labeled ethylene dicysteine (EC) is a well-established agent for renal tubular function imaging, the use of [(188)Re] rhenium-labeled EC as a potential agent for prevention of restenosis after angioplasty is worth evaluation. In this article, the preparation and pharmacological behavior of [(188/186)Re]Re complex of EC are reported. The yield of the Re complex was optimized by varying the parameters of complexation. The complex prepared under the optimized conditions was found to be stable over a period of 7 days when stored at pH 2 and at 4 degrees C. The pharmacological behavior of [(188/186)Re]Re-EC confirms its similarity to (188)Re-MAG(3) and its superiority over (188)ReO(4)(-) for use in endovascular brachytherapy.

摘要

188ReO(4)(-)、(188)Re-MAG(3)和(188)Re-DTPA目前正作为用于冠状动脉成形术后预防再狭窄的充液球囊中的辐射源进行研究。由于(99m)Tc标记的乙二胱氨酸(EC)是一种成熟的肾小管功能成像剂,因此使用[(188)Re]铼标记的EC作为血管成形术后预防再狭窄的潜在药物值得评估。本文报道了EC的[(188/186)Re]铼配合物的制备及药理行为。通过改变络合参数优化了铼配合物的产率。在优化条件下制备的配合物在pH 2和4℃下储存7天期间被发现是稳定的。[(188/186)Re]Re-EC的药理行为证实了其与(188)Re-MAG(3)的相似性及其在血管内近距离治疗中优于(188)ReO(4)(-)的特性。

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