High affinity ligands for the imaging of serotonin transporter: 4-halo-6-nitroquipazine derivatives

초록

After understanding of dopamine transporter, imaging of serotonin (5-hydoxytryptamine or 5-HT) reuptake sites in the mammalian brain using PET and SPECT is an active and emerging research field. 6-Nitroquipazine (Ki = 0.17 nM) has the high binding affinity toward 5-HT transporter (SERT), but structure-activity relationship (SAR) of its derivatives has not been extensively studied. A number of 6-nitroquipazine derivatives are synthesized and some of the new ligands have high affinities for SERT. Affinities of these compounds will be reported including one having 17 pmol binding. Labeling as well as SAR will also be presented.