Design of a radiopharmaceutical for the palliation of painful bone metastases: rhenium-186-labeled bisphosphonate derivative
Design of a radiopharmaceutical for the palliation of painful bone metastases: rhenium-186-labeled bisphosphonate derivative
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DOI：
10.1002/jlcr.864
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发表时间：
2004-10-15
影响因子：
1.8
通讯作者：
Saji, H
中科院分区：
文献类型：
--
作者：
Ogawa, K;Mukai, T;Saji, H
为了开发一种用于缓解骨转移癌疼痛的放射性药物，基于双功能放射性药物的概念，我们设计了一种固定在稳定的Re-186-单氨基单氨基二硫醇(MAMA-BP)上的双膦酸衍生物(Re-186-MAMA-BP)以改善Re-186-HEDP的不稳定性。通过将Tr-MAMA衍生物的羧基与双膦酸衍生物的氨基偶联，合成了Re-186-MAMA-BP的前体(Tr-MAMA-BP)。以Re-186-葡庚糖酸酯为原料，通过配体交换反应合成了Re-186标记化合物，放化产率为32.0+/-4.1%。在pH 7.0的缓冲溶液中，Re-186-MAMA-BP比Re-186-HEDP更稳定。这表明Re-186-MAMA-BP是一种潜在的缓解骨转移疼痛的放射性药物。版权所有(C)2004 John Wiley Sons，Ltd.
To develop a radiopharmaceutical for the palliation of painful bone metastases based on the concept of bifunctional radiopharmaceuticals, we designed a bisphosphonate derivative attached to a stable Re-186-monoaminemonoamidedithiol (MAMA) chelate (Re-186-MAMA-BP) to improve the instability of Re-186-HEDP. The precursor (Tr-MAMA-BP) of Re-186-MAMA-BP was synthesized by coupling the carboxyl group of the Tr-MAMA derivative with the amino group of the bisphosphonate derivative. This Re-186-labeled compound was prepared by a ligand exchange reaction using Re-186-glucoheptonate with a radiochemical yield of 32.0 +/- 4.1%. In the incubation study in buffered solution (pH 7.0), Re-186-MAMA-BP was more stable than Re-186-HEDP. This suggests that Re-186-MAMA-BP is a potential radiopharmaceutical for the palliation of painful bone metastases. Copyright (C) 2004 John Wiley Sons, Ltd.