Article
Synthesis and inhibitory evaluation of 3-linked imipramines for the exploration of the S2 site of the human serotonin transporter.
Bioorganic & medicinal chemistry - 15 Jun 2016
Brinkø Anne, Larsen Maja T, Koldsø Heidi, Besenbacher Louise, Kolind Anders, Schiøtt Birgit, Sinning Steffen, Jensen Henrik H
Abstract excerpt
The human serotonin transporter is the primary target of several antidepressant drugs, and the importance of a primary, high affinity binding site (S1) for antidepressant binding is well documented. The existence of a lower affinity, secondary binding site (S2) has, however, been debated. Herein we report the synthesis of 3-position coupled imipramine ligands from clomipramine using a copper free Sonogashira...
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