Article
Structure-activity relationship studies of citalopram derivatives: examining substituents conferring selectivity for the allosteric site in the 5-HT transporter.
British journal of pharmacology - 1 Mar 2016
Larsen M Andreas B, Plenge Per, Andersen Jacob, Eildal Jonas N N, Kristensen Anders S, Bøgesø Klaus P, Gether Ulrik, Strømgaard Kristian, Bang-Andersen Benny, Loland Claus J
Abstract excerpt
BACKGROUND AND PURPOSE: The 5-HT transporter (SERT) is a target for antidepressant drugs. SERT possesses two binding sites: the orthosteric (S1) binding site, which is the presumed target for current SERT inhibitors, and an allosteric (S2) site for which potential therapeutic effects are unknown. The antidepressant drug citalopram displays high-affinity S1 binding and low-affinity S2 binding. To elucidate a...
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