【文章名】From the Selective Serotonin Transporter Inhibitor Citalopram to the Selective Norepinephrine Transporter Inhibitor Talopram: Synthesis and Structure-Activity Relationship Studies.
From the Selective Serotonin Transporter Inhibitor Citalopram to the Selective Norepinephrine Transporter Inhibitor Talopram: Synthesis and Structure-Activity Relationship Studies.
作者
Eildal, Jonas N. N.;Andersen, Jacob;Kristensen, Anders S.;Jorgensen, Anne Marie;Bang-Andersen, Benny;Jorgensen, Morten;Stromgaard, Kristian;
[摘要]：Citalopram and talopram are structurally closely related, but they have very distinct pharmacol. profiles as selective inhibitors of the serotonin and norepinephrine transporters, resp. A systematic structure-activity relationship study was performed, in which each of the four positions distinguishing the two compds. were varied. The inhibitory potencies of the resulting 16 compds. were tested at both serotonin and norepinephrine transporters. This showed that particularly two of the four positions are determinants for the biol. activity.
