Synthesis of several MPP derivatives for ^(99m)Tc-labelling and evaluated as potential 5-HT_(1A) receptor imaging agents  

作　　者：YANG WenJiang LIN Yan ZHANG XianZhong ZHANG JunBo WANG XueBin 

机构地区：[1]Key Laboratory of Radiopharmaceuticals(Beijing Normal University),Ministry of Education,College of Chemistry,Beijing Normal University,Beijing 100875,China

出　　处：《Science China Chemistry》2011年第7期1148-1154,共7页中国科学(化学英文版)

基　　金：supported by the National Natural Science Foundation of China (20401004);the Fundamental Research Funds for the Central Universities of China

摘　　要：The(2-methoxyphenyl) piperazine(MPP) was selected as the functional group and conjugated to dithiocarbamate through different spacers.A series of new MPP derivatives(MPPnDTC,n = 2-6) were synthesized and radiolabelled with 99mTc-nitrido core or 99mTc-tricarboxyl core as potential 5-HT1A receptor imaging agents.All the six 99mTc-labelled complexes were lipophilic and neutral.Biodistribution results showed that those radiotracers had moderate initial brain and hippocampus uptake.There have no significant relation was observed between the biological properties of these tracers with the length of its carbon chain.The radioactivity concentrations of hippocampus of 99mTcN-MPP2DTC,99mTcN-MPP3DTC,99mTcN-MPP4DTC,99mTcN-MPP5DTC,99mTcN-MPP6DTC and 99mTc(CO)3-MPP3DTC at 2 min post-injection time(p.i.) were 0.43,1.15,0.99,1.04,1.13 and 0.83 %ID/g,respectively.The (2-methoxyphenyl) piperazine (MPP) was selected as the functional group and conjugated to dithiocarbamate through different spacers. A series of new MPP derivatives (MPPnDTC, n = 2-6) were synthesized and radiolabelled with 99mTc-nitrido core or 99mTc-tricarboxyl core as potential 5-HT1A receptor imaging agents. All the six 99mTc-labelled complexes were lipophilic and neutral. Biodistribution results showed that those radiotracers had moderate initial brain and hippocampus uptake. There have no significant relation was observed between the biological properties of these tracers with the length of its carbon chain. The radioactivity concentrations of hippocampus of 99mTcN-MPP2DTC, 99mTcN-MPP3DTC, 99mTcN-MPP4DTC, 99mTcN- MPP5DTC, 99mTcN-MPP6DTC and 99mTc(CO)3-MPP3DTC at 2 min post-injection time (p.i.) were 0.43, 1.15, 0.99, 1.04, 1.13 and 0.83 %ID/g, respectively.

关 键 词：MPP 99mTc-nitrido core 99mTc-tricarboxyl core 5-HT_(1A) receptor 

分 类 号：O621.2[理学—有机化学]