Primary study of a novel Tc-tricarbonyl cocaine analogue as the potential DAT imaging agent

The convenient preparation of organometallic precursor fac-99mTc(CO)3 (H2O)3] opens a new route to design new radiopharmaceuticals. Based on this precursor, a new cocaine analogue, Tropyn, is designed and synthesized,and “2 1” mixed-ligands approach is used to prepare a neutral complex ^99mTc(CO)3(Tropyn)I]. Biodistribution in mice and rats proves that it has sufficient brain uptake. Rat regional brain biodistribntion indicates that the complex is highly concentrated in the striatum (ST) with rapid clearance in the cortex (CT) and hippocampus (HP), which make it valuable for further investigation as the potential Second-Generation DAT imaging agent.

Primary study of a novel Tc-tricarbonyl cocaine analogue as the potential DAT imaging agent

The convenient preparation of organometallic precursor fac-^99mTc(CO)₃ (H²O)₃]⁺ opens a new route to design new radiopharmaceuticals. Based on this precursor, a new cocaine analogue, Tropyn, is designed and synthesized, and “2+1” mixed-ligands approach is used to prepare a neutral complex ^99mTc(CO)₃(Tropyn)I]. Biodistribution in mice and rats proves that it has sufficient brain uptake. Rat regional brain biodistribution indicates that the complex is highly concentrated in the striatum (ST) with rapid clearance in the cortex (CT) and hippocampus (HP), which make it valuable for further investigation as the potential Second-Generation DAT imaging agent.