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}
}
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366 Citations
Highly Influential Citations
24
Background Citations
110
Methods Citations
15
Results Citations
12

366 Citations

[Escitalopram: a selective inhibitor and allosteric modulator of the serotonin transporter].
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.
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.
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.
L’escitalopram : un inhibiteur sélectif et un modulateur allostérique du transporteur de la sérotonine
Pharmacological properties of the active metabolites of the antidepressants desipramine and citalopram.
Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity
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
Managing depressive and anxiety disorders with escitalopram
  • M. Thase
  • Psychology
    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).
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.
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