Shukla Gauri, Tiwari Anjani K, Sinha Deepa, Srivastava Rakesh, Cahndra Hairsh, Mishra Anil K
Department of Cyclotron and Radiopharmaceutical Sciences, INMAS, Delhi, India.
Cancer Biother Radiopharm. 2009 Apr;24(2):209-14. doi: 10.1089/cbr.2008.0551.
Indole-based alendronate (AI) was derived from the condensation reaction of indole 3-carboxaldehyde with sodium alendronate (ALN) and was characterized by various spectroscopic methods (e.g., ultraviolet, fourier-transform-infrared, and liquid chromatography mass spectrometry). The AI was labeled with (99m)Tc and radiochemical purity was above 97%, which was ascertained by instant thin-layer chromatography, using different solvent conditions, with a specific activity 2-5 mCi/mg. The receptor ligand assay on human bone cell line Soas-2 showed K(D) = 0.55 nM. The derivative (AI) was stable, which was determined under physiologic conditions up to 24 hours The blood kinetic study showed a biexponential pattern as well as quick wash-out from the circulation with varying biologic t(1/2)(F) and t(1/2)(S). Excellent-quality radio images were recorded of bone, showing a rapid clearance of background activity, at an early visualization at 1.5 hours. The excretory pathway of the derivative was through the kidneys, which was evidenced by biodistribution studies. Thus, the newly synthesized derivative can be considered as a specific bone-seeking agent.
基于吲哚的阿仑膦酸盐（AI）由吲哚 - 3 - 甲醛与阿仑膦酸钠（ALN）缩合反应制得，并通过多种光谱方法（如紫外、傅里叶变换红外和液相色谱质谱）进行表征。AI用（99m）Tc标记，放射化学纯度高于97%，这通过即时薄层色谱法在不同溶剂条件下测定，比活度为2 - 5 mCi/mg。对人骨细胞系Soas - 2的受体配体分析显示解离常数K(D)=0.55 nM。该衍生物（AI）在生理条件下长达24小时是稳定的。血液动力学研究显示出双指数模式以及从循环中快速清除，具有不同的生物半衰期t(1/2)(F)和t(1/2)(S)。在1.5小时的早期显像时，记录到了高质量的骨骼放射性图像，显示背景活性快速清除。该衍生物的排泄途径是通过肾脏，这在生物分布研究中得到了证实。因此，新合成的衍生物可被视为一种特异性亲骨剂。
