一种新型骨显像剂^(99m)TcAMDP的初步研究

A PRELIMINARY STUDY ON A NEW KIND OF BONE IMAGING AGENT^(99m)Tc AMDP

以二苄胺、原甲酸三乙酯和亚磷酸二乙酯为原料 ,经过加热回流、催化还原、酸性水解等反应合成了亚甲基氨基二膦酸 (AMDP)配体 .通过熔点、元素分析和1 HNMR测定进行了结构确认 ;研究了SnCl2 的量、pH变化对 99mTc标记AMDP的影响 ,选择 2种层析条件对标记率进行测定 ,在所选择的标记条件下 ,标记率高于 95% .进行了小鼠体内分布实验 ,并与99mTc MDP进行对比 ,结果表明99mTc AMDP与99mTc MDP均具有较强的亲骨性能 ,99mTc AMDP的肺、肝、脾等的摄取率高于99mTc MDP ,而其初期骨摄取率则明显高于99mTc MDP ,初期骨与肌肉、骨与血的摄取率比要好于99mTc MDP ,是一种值得深入研究的新型骨显像剂 .

Aminobisphosphonate(AMDP) is prepared from dibenzylamine, triethyl orthoformate and diethyl phosphite by refluxing, reducing and acid hydrolysis. Its structure is determined by melting point, elemental analysis and 1 HNMR.The effects of the concentration of SnCl 2·2H 2O and pH value on labelling of AMDP with 99m Tc are investigated. The labelling yields of 99m Tc AMDP is more than 95% under the selected labelling condition. The biodistribution of 99m Tc AMDP is studied in mice and contrasted with 99m Tc MDP. The results demonstrate that 99m Tc AMDP and 99m Tc MDP all have high bone uptake. The lung, liver and spleen uptake of 99m Tc AMDP is clearly higher than 99m Tc MDP,but the initial bone uptake of 99m Tc AMDP is obviously higher than 99m Tc MDP and the ratios of bone and muscle, bone and blood of 99m Tc AMDP are also higher than 99m Tc MDP. Therefore, 99m Tc AMDP is probably a new kind of bone imaging agent and further study is needed.