The interaction of escitalopram and R-citalopram at the human serotonin transporter investigated in the mouse.

ABSTRACT:

Rationale

Escitalopram appears to be a superior antidepressant to racemic citalopram. It has been hypothesized that binding of R-citalopram to the serotonin transporter (SERT) antagonizes escitalopram binding to and inhibition of the SERT, there by curtailing the elevation of extracellular 5-hydroxytryptamine (5-HTExt), and hence anti-depressant efficacy. Further, it has been suggested that a putative allosteric binding site is important for binding of escitalopram to the primary, orthosteric, site, and for R-citalopram's inhibition here of.

Objectives

Primary: Investigate at the human (h)SERT, at clinical relevant doses, whether R-citalopram antagonizes escitalopram-induced 5-HTExt elevation. Secondary: Investigate whether abolishing the putative allosteric site affects esc

SUBMITTER: Jacobsen JP 

PROVIDER: S-EPMC4346315 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature