Fluoxetine: a case history of its discovery and preclinical development

@article{PerezCaballero2014FluoxetineAC,
  title={Fluoxetine: a case history of its discovery and preclinical development},
  author={L Perez-Caballero and Sonia Alejandra Torres-S{\'a}nchez and Lidia Bravo and Juan Antonio Mic{\'o} and Esther Berrocoso},
  journal={Expert Opinion on Drug Discovery},
  year={2014},
  volume={9},
  pages={567 - 578}
}
Introduction: Depression is a multifactorial mood disorder with a high prevalence worldwide. Until now, treatments for depression have focused on the inhibition of monoaminergic reuptake sites, which augment the bioavailability of monoamines in the CNS. Advances in drug discovery have widened the therapeutic options with the synthesis of so-called selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine. Areas covered: The aim of this case history is to describe and discuss the… 
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References

SHOWING 1-10 OF 119 REFERENCES
Clinical effects of serotonin reuptake inhibitors in the treatment of depressive illness.
TLDR
Evidence suggests that, compared with tricyclic antidepressants, these drugs may cause fewer anticholinergic effects and lower cardiotoxicity in the treatment of major depressive disorders and these drugs will undoubtedly provide important insights into depressive illness and some anxiety disorders and may fulfill their initial promise.
Neurotrophins Role in Depression Neurobiology: A Review of Basic and Clinical Evidence
TLDR
Preclinical and clinical studies aimed at disclosing the role of neurotrophins in the pathophysiological mechanisms of depression and the mode of action of antidepressants, which favour the neurotrophic/neurogenic hypothesis are reviewed.
Clinical pharmacokinetics of selective serotonin reuptake inhibitors.
TLDR
No convincing evidence exists of a relationship between plasma concentrations of any of the SSRIs and clinical efficacy, and available data indicate that metabolism ofSSRIs is impaired with reduced liver function.
Pharmacological characterization of selective serotonin reuptake inhibitors (SSRIs)
  • J. Hyttel
  • Psychology, Biology
    International clinical psychopharmacology
  • 1994
TLDR
Since the marketed SSRIs all show clear antidepressant effect, this receptor regulation seems not to be a prerequisite for clinical antidepressant activity.
microRNAs as novel antidepressant targets: converging effects of ketamine and electroconvulsive shock therapy in the rat hippocampus.
TLDR
Investigating changes to hippocampal miRNA levels induced via early-life stress in Sprague-Dawley rats and whether antidepressant treatments could reverse these changes demonstrates that changes to hippocampusal miRNAs may represent an important component of stress-induced pathology and antidepressant action may reverse these.
Effects of Chronic Fluoxetine in Animal Models of Anxiety and Depression
TLDR
Several novel effects of chronic, but not subchronic, antidepressant treatment are presented, including increased swimming and reduced immobility in the forced swim test and anxiety-related measures were reduced by 18 mg/kg/day.
Antipanic-like effect of serotonin reuptake inhibitors in the elevated T-maze
Clinical Pharmacology and Pharmacokinetics of Fluoxetine: A Review
TLDR
This paper reviews the published information relevant to fluoxetine's pharmacology and pharmacokinetics in man and describes it as one of the first selective serotonin uptake inhibitors.
Comparison of the Effects of Antidepressants and Their Metabolites on Reuptake of Biogenic Amines and on Receptor Binding
TLDR
The present survey compares the effects of antidepressants and their principal metabolites on reuptake of biogenic amines and on receptor binding to suggest that both dopaminergic and noradrenergic components play a role and that the hydroxybupropion metabolite contributes significantly to the antidepressant activity.
...
1
2
3
4
5
...