3-氨-1-羟丙基-1,1-二膦酸盐的<sup>131</sup>I标记化合物的合成及其初步动物实验

3-氨-1-羟丙基-1,1-二膦酸盐的¹³¹I标记化合物的合成及其初步动物实验

摘要: 合成了3-氨-1-羟丙基-1,1-二膦酸二钠水合物(ABP)配体，并以5-(三正丁基锡)-3-吡啶甲酸-N-琥珀酰亚胺酯(SPC)为双功能偶联剂，进行了¹³¹I标记的研究。其标记率大于64%，放化纯度大于99%。室温下，标记产物放置72 h后，放化纯度仍大于98.8%。初步动物实验结果表明，标记产物¹³¹I-SIPC-ABP对小鼠骨骼具有明显的亲和力，具有较高的体内外稳定性。

Abstract: 3-amino-1-hydroxypropylidene-1,1-bisphosphonate (ABP) was synthesized and labeled with ¹³¹I using N-succinimidyl-5-(tri-butylstannyl)-3-pyridinecarboxylate(SPC) as a bi-functional linker. ¹³¹I could be coupled to ABP via a ¹³¹I-SIPC intermediate with a labeling yield of more than 64%, and a radiochemical purity of more than 99% after HPLC purification. After72 h at room temperature, the radiochemical purity was still more than 98.8%, implying that the ¹³¹I-SIPC-ABP is stable in vitro. Biodistribution experiments in mice show that ¹³¹I-SIPC-ABP has high affinity to bone and high stability in vivoas well as in vitro.