论文部分内容阅读
为了寻找 99Tcm 标记中枢神经系统 5 - HT1A协同受体显像药物 ,合成了单齿受体配基 1- (2 -甲氧基苯基 ) - 4 - (2 -巯基乙基 )哌嗪 (简称 MPMEP)、三齿配体 N,N-二 (2 -巯基乙基 ) - N’,N’-二乙基乙二胺 (简称 BMPDEEDA)和 N,N-二 (2 -巯基乙基 )卞胺 (简称 BMPBA) ,其结构经 IR、NMR及元素分析表征 ;以“3+ 1”混合配体进行了 99Tcm标记 ,并确定了标记反应的最佳条件 :p H=6 .0～ 7.0 ,6 0～70℃下 ,反应 2 0～ 30 min,经 CH2 Cl2 萃取脂溶性部分后 ,99Tcm O(MPMEP) (BMPDEEDA)和 99Tcm O(MPMEP) (BMPBA)的标记率分别达到 95 %和 90 %以上。采用 HPL C对标记产物进行了分离和纯化 ,纯化后的标记物放化纯度均 >98%。小鼠体内的生物分布结果表明 99Tcm O(MPMEP)(BMPDEEDA)和 99Tcm O(MPMEP) (BMPBA)配合物可以通过血脑屏障 ,在脑中有一定的摄取和滞留 ;99Tcm O(MPMEP) (BMPBA)在血液中清除较快 ,静脉注射后 2、30、6 0 min时 ,脑与血摄取比分别为 0 .31、0 .33、0 .32 ,但血液中放射性活度仍然较高
In order to find a 99Tcm labeled central nervous system 5 - HT1A co - receptor imaging drug, the monodentate ligand ligand 1- (2 - methoxyphenyl) -4 - (2 - mercaptoethyl) MPMEP), tridentate ligand N, N-bis (2-mercaptoethyl) -N ’, N’- diethylethylenediamine (BMPDEEDA) and N, (BMPBA). Its structure was characterized by IR, NMR and elemental analysis. The 99Tcm labeling was carried out with a mixed ligand of “3+ 1” and the optimal conditions for labeling reaction were determined: p H = 6.0-7.0, The labeling rates of 99TcmO (BMPDEEDA) and 99TcmO (BMPMEP) (BMPBA) reached 95% and 90% respectively after the lipophilic fractions were extracted with CH 2 Cl 2 at 60-70 ℃ for 20-30 min. the above. The labeled product was isolated and purified using HPL C, and the radiochemical purity of the purified product was> 98%. The biodistribution results in mice showed that 99Tcm O (MPMPE) (BMPDEEDA) and 99Tcm O (MPMEP) (BMPBA) complexes could pass through the blood-brain barrier with some uptake and retention in the brain. ) Was rapidly cleared in the blood. At 2, 30 and 60 min after intravenous injection, the brain-to-blood uptake ratios were 0.31, 0.33, 0.32, respectively, but the radioactivity in the blood was still high