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...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.展开更多
基金supported by the National Natural Science Foundation of China (20401004)the Fundamental Research Funds for the Central Universities of China
文摘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.
