Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine

@article{Owens2001SecondgenerationSH,
  title={Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine},
  author={Michael J. Owens and David L. Knight and Charles B. Nemeroff},
  journal={Biological Psychiatry},
  year={2001},
  volume={50},
  pages={345-350}
}
BACKGROUND Single isomers of the selective serotonin reuptake inhibitors citalopram (escitalopram, S-citalopram) and fluoxetine (R-fluoxetine) are currently under development for the treatment of depression and other psychiatric disorders. Previous studies conducted in laboratory animals have revealed that the biological effects on serotonin reuptake for citalopram reside in the S enantiomer. In contrast, both enantiomers of fluoxetine contribute to its biological activity. METHODS In the… Expand
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[Escitalopram: a selective inhibitor and allosteric modulator of the serotonin transporter].
TLDR
Citalopram exerts a stabilizing effect on this association to SERT, resulting in an effective inhibition of 5-HT reuptake activity, and an allosteric interaction between the enantiomers and the 5- HT transporter (SERT) has been proposed. Expand
PET measurement of serotonin transporter occupancy: a comparison of escitalopram and citalopram.
TLDR
The small but significant difference in occupancy and K(i),(app) found between R,S-citalopram and S-cITALopram suggests that not only S- citaloprams but also R-citalsopram to some degree occupies the 5-HTT in the human brain in vivo. Expand
Escitalopram: A Second-Generation SSRI
TLDR
Escitalopram is a promising candidate for use as a first-line antidepressant because of its receptor binding properties and activity in preclinical animal models of depression, and because of the most selective SSRI yet developed. Expand
The interaction of escitalopram and R-citalopram at the human serotonin transporter investigated in the mouse
TLDR
No evidence is found that R-citalopram directly antagonizes escitalo-induced 5-HTExt elevation or that the putative allosteric site is important for hSERT inhibition by escITALopram. Expand
L’escitalopram : un inhibiteur sélectif et un modulateur allostérique du transporteur de la sérotonine
Citalopram (Seropram) is an antidepressant of the selective serotonin (5-HT) reuptake inhibitor (SSRI) class, composed of equal amounts of S-enantiomer, escitalopram, and R-enantiomer, R-citalopram.… Expand
Pharmacological properties of the active metabolites of the antidepressants desipramine and citalopram.
TLDR
The pharmacological effects of desipramine in rats may be attributed not only to the inhibition of the norepinephrine transporter by desipramsine but also toThe inhibition of serotonin transporter by the active metabolite desmethyldesipramines. Expand
Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity
TLDR
Milnacipran's binding and uptake inhibition profile more closely resembles that of the tricyclic antidepressants than that of duloxetine and whether these differences observed in vitro manifest themselves in vivo is not clear. Expand
The S-enantiomer of R,S-citalopram, increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors
TLDR
Escitalopram shows a unique interaction with the hSERT compared with other 5-HT reuptake inhibitors (SSRIs) and displays a pronounced effect via an affinity-modulating allosteric site that stabilised the [3H]-escITALopram/SERT complex via anallosteric effect at a low-affinity binding site. Expand
Managing depressive and anxiety disorders with escitalopram
  • M. Thase
  • Medicine
  • Expert opinion on pharmacotherapy
  • 2006
TLDR
Pharmacoeconomic models suggest that the greater drug acquisition cost of this patent-protected compound may be offset by greater efficacy (relative to generic citalopram) and tolerability (compared with extended release venlafaxine). Expand
Investigating the Potential Role of Serotonin-2B Receptor Antagonism in the Neuronal Actions of Adjunctive Aripiprazole
TLDR
5-HT2B receptor blockade rescues an SSRI-mediated decrease in DA firing activity and increases mPFC pyramidal neuron firing and bursting activity mediated by aripiprazole and in combination with escitalopram may be, at least partly, moderated by 5- HT2B receptors expressed in this brain area. Expand
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