Synthesis radiolabeling and baboon SPECT imaging of 2β-carbomethoxy-3β-(3′-123Iiodophenyl)tropane (123IYP256) as a serotonin transporter radiotracer.(123IYP256) a potential serotonin transporter radiotracer)

摘要

To develop a potential SPECT probe to evaluate the integrity of the serotoninergic system (5-HTT) whose dysfunction is linked to several disease conditions such as Parkinson’s, Alzheimer’s diseases and depression, we report the synthesis, radiolabeling and in vivo baboon imaging of 2β-carbomethoxy-3β-(3′-[¹²³I]iodophenyl) tropane (>YP256, >6). The radiolabeling was performed by iododestannylation using sodium [¹²³I]iodide and peracetic acid. Although the ligand displayed high selectivity for 5-HTT over dopamine transporter (DAT) in vitro, SPECT imaging in baboons did not reveal selective 5-HTT accumulation in brain in vivo.