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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 neu- tral complex [99mTc(CO)3(Tropyn)I]. Biodistribution in mice and rats proves that it has sufficient brain uptake. Rat re- gional brain biodistribution indicates that the complex is highly concentrated in the striatum (ST) with rapid clear- ance in the cortex (CT) and hippocampus (HP), which make it valuable for further investigation as the potential Sec- ond-Generation 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 neu-tral complex [99mTc (CO) 3 (Tropyn) I]. Biodistribution in mice and rats proves that it has sufficient brain uptake. Rat re- gional brain biodistribution that that the complex is highly concentrated in the striatum (ST) with rapid clear-ance in the cortex (CT) and hippocampus (HP), which make it valuable for further investigation as the potential Sec-ond-Generation DAT imaging agent.