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

  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},
PET measurement of serotonin transporter occupancy: a comparison of escitalopram and citalopram.
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
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
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.
Managing depressive and anxiety disorders with escitalopram
  • M. Thase
  • Psychology
    Expert opinion on pharmacotherapy
  • 2006
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
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.


Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors.
The new antidepressant drugs, fluoxetine (and its enantiomers), citalopram, indalpine, paroxetine, and femoxetine show relatively weak affinities for 5-HT receptors as measured by radioligand binding
Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.
Novel findings, not widely described previously, suggest that many of the individual drugs studied in these experiments possess some structural characteristic that determines affinity for several G protein-coupled, but not muscarinic, receptors.
Absolute configurations and pharmacological activities of the optical isomers of fluoxetine, a selective serotonin-uptake inhibitor.
The goals of this study were to determine the absolute configurations of the enantiomers of fluoxetine and to examine whether the actions of fluxetine in behavioral tests were enantiospecific, and to ensure that the eudismic ratio for the fluoxettine enantiomer is near unity.
Blockage of 5HT2C serotonin receptors by fluoxetine (Prozac).
  • Y. Ni, R. Miledi
  • Biology, Psychology
    Proceedings of the National Academy of Sciences of the United States of America
  • 1997
The results show that fluoxetine is a competitive and reversible antagonist of 5HT2C receptors and suggest that some therapeutic effects of fluoxettine may involve blockage of 5 HT receptors, in addition to its known blockage to 5HT transporters.
Interaction of the enantiomers of fluoxetine and norfluoxetine with human liver cytochromes P450.
The data indicate that the enantiomers of fluoxetine and norfluoxetines are potent inhibitors of P450 2D6 and that P450 forms other than P4502D6 appear to be responsible for the majority of microsomal fluoxettine N-demethylation.
Plasma levels of citalopram enantiomers and metabolites in elderly patients.
It is hypothesized that quantification of S(+) citalopram will permit a more accurate examination of dose/response relationships, and seems to be especially important for older subjects, given the wide ranges and higher concentrations evident from preliminary results.
Identification of three cytochrome P450 isozymes involved in N-demethylation of citalopram enantiomers in human liver microsomes.
The results confirm that the use of cDNA expressed CYP isozymes is a potent tool for the measurement of kinetic constants and help to predict clearance modifications of CIT enantiomers, especially in poor metabolizers of mephenytoin or patients comedicated with potent CYP2C19 or 3A4 inhibitor(s).