不同中心核锝99m标记CPeI配合物的制备与生物分布

THE PREPARATION AND BIODISTRIBUTION OF CYCLOPENTYLISONITRILE COMPLEXES LABELED WITH DIFFERENT TECHNETIUM-99m CORES

以环戊胺为原料 ,通过甲酰胺化和脱水 2步反应制得配体环戊基异腈 (CPeI) ,对其进行了熔、沸点测定 ,红外和元素分析等表征 ,并通过不同方法进一步得到 3种不同中心核的99mTc标记配合物 :99mTc CPeI,99mTcN CPeI和99mTc(CO) 3 CPeI .3种配合物均为脂溶性 ,在室温下放置 6h以上放化纯无明显变化 .在正常昆明小鼠体内进行的生物分布实验结果表明 :3种配合物均有一定的心肌摄取 ,但肝本底均较高 ;99mTc(CO) 3 CPeI的肺摄取要明显低于99mTc CPeI和99mTcN CPeI,且清除速度也相当快 ;99mTc CPeI的血本底相对较低且清除最快 ,99mTc(CO) 3 CPeI次之 ,99mTcN CPeI的血本底最高且清除最慢 .3种配合物生物分布的显著差异显示了不同中心核对配合物生物性能的影响 ,因此可以利用已知配体通过不同标记方法制得具有不同中心核的配合物 。

An isonitrile ligand cyclopentylisonitrile (CPeI) is synthesized and a copper salt \[Cu(I)(CPeI) 4 BF 4 \] of this ligand is also prepared. The isonitrile and its copper salt are characterized by IR and elemental analysis. These lipophilic complexes labeled with different 99m Tc cores are expressed as 99m Tc(CO) 3 CPeI, 99m TcN CpeI and 99m Tc CPeI, respectively. The results of stability study indicate that these complexes are all stable over a period of 6 h at room temperature. The biodistribution of these complexes in mice indicates that they have some myocardial uptake, but they are all mainly accumulated in liver. The uptake of 99m Tc(CO) 3 CPeI in lung and blood is less than that of the other two complexes. 99m Tc(CO) 3 CPeI is the best one for myocardial perfusion imaging although it has no promising properties. These complexes with different cores have significantly different uptake properties in most tissues. It is an effective route to find new radiopharmaceuticals by using a known ligand labeled with different cores.