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A selective serotonin reuptake enhancer (SSRE) is a type of drug which enhances the plasmalemmal reuptake of the neurotransmitter serotonin, leading to a decrease in its synaptic concentrations and therefore a decrease in serotonergic neurotransmission.[1]

The only known drug of this class is tianeptine, which while structurally related to the tricyclic antidepressants has an entirely distinct mechanism of action. The precise mechanism of action of tianeptine remains unclear despite several decades of research and clinical use, and while it has been speculated that tianeptine might act as an allosteric modulator of the serotonin transporter at a separate site to that used by SSRIs, newer research suggests that its direct action is actually alteration of AMPA glutamate receptor activity, which then leads to enhanced serotonin reuptake via a downstream mechanism which has yet to be fully characterised, but seems to involve altered neuroplasticity and release of BDNF.[2][3][4][5][6][7][8][9]

SSREs are used as antidepressants for the treatment of depression and anxiety, and are in marked contrast to other antidepressants such as the selective serotonin reuptake inhibitors (SSRIs), which inhibit the reuptake of serotonin instead.[1][10] SSREs have been demonstrated to be as effective as SSRIs against depression, have a much faster onset of action (immediate), and have a much better tolerability profile,[1][10] although interestingly, it has also been shown that the SSRI fluoxetine can substitute for tianeptine in animal studies.[11]

The only currently known and available SSRE is tianeptine (Stablon, Coaxil, Tatinol) and while several related compounds are disclosed in the original patent,[12] it is unclear whether these share tianeptine's unique pharmacological effects, as amineptine, the most closely related drug to have been widely studied, is a dopamine reuptake inhibitor with no significant effect on serotonin levels, and conversely tianeptine has no affinity for the dopamine transporter.

See also

References

  1. ^ a b c Mennini T, Mocaer E, Garattini S. (1987). "Tianeptine, a selective enhancer of serotonin uptake in rat brain.". Naunyn Schmiedebergs Arch Pharmacol. 336 (5): 478–482. PMID 3437921.  
  2. ^ Kole MH, Swan L, Fuchs E (September 2002). "The antidepressant tianeptine persistently modulates glutamate receptor currents of the hippocampal CA3 commissural associational synapse in chronically stressed rats". The European Journal of Neuroscience 16 (5): 807–16. PMID 12372016. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0953-816X&date=2002&volume=16&issue=5&spage=807.  
  3. ^ McEwen BS, Chattarji S (December 2004). "Molecular mechanisms of neuroplasticity and pharmacological implications: the example of tianeptine". European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology 14 Suppl 5: S497–502. doi:10.1016/j.euroneuro.2004.09.008. PMID 15550348.  
  4. ^ McEwen BS, Olié JP (June 2005). "Neurobiology of mood, anxiety, and emotions as revealed by studies of a unique antidepressant: tianeptine". Molecular Psychiatry 10 (6): 525–37. doi:10.1038/sj.mp.4001648. PMID 15753957.  
  5. ^ Brink CB, Harvey BH, Brand L (January 2006). "Tianeptine: a novel atypical antidepressant that may provide new insights into the biomolecular basis of depression". Recent Patents on CNS Drug Discovery 1 (1): 29–41. PMID 18221189. http://www.bentham-direct.org/pages/content.php?PRN/2006/00000001/00000001/0002PRN.SGM.  
  6. ^ Svenningsson P, Bateup H, Qi H, Takamiya K, Huganir RL, Spedding M, Roth BL, McEwen BS, Greengard P (December 2007). "Involvement of AMPA receptor phosphorylation in antidepressant actions with special reference to tianeptine". The European Journal of Neuroscience 26 (12): 3509–17. doi:10.1111/j.1460-9568.2007.05952.x. PMID 18088278.  
  7. ^ Kasper S, McEwen BS (2008). "Neurobiological and clinical effects of the antidepressant tianeptine". CNS Drugs 22 (1): 15–26. PMID 18072812.  
  8. ^ Bobula B, Hess G (2008). "Antidepressant treatments-induced modifications of glutamatergic transmission in rat frontal cortex". Pharmacological Reports : PR 60 (6): 865–71. PMID 19211978. http://www.if-pan.krakow.pl/pjp/pdf/2008/6_865.pdf.  
  9. ^ Qi H, Mailliet F, Spedding M, Rocher C, Zhang X, Delagrange P, McEwen B, Jay TM, Svenningsson P (January 2009). "Antidepressants reverse the attenuation of the neurotrophic MEK/MAPK cascade in frontal cortex by elevated platform stress; reversal of effects on LTP is associated with GluA1 phosphorylation". Neuropharmacology 56 (1): 37–46. doi:10.1016/j.neuropharm.2008.06.068. PMID 18657555.  
  10. ^ a b Defrance R, Marey C, Kamoun A. (1988). "Antidepressant and anxiolytic activities of tianeptine: an overview of clinical trials.". Clin Neuropharmacol. 11 (2): S74-82. PMID 2902922.  
  11. ^ Alici T, Kayir H, Aygoren MO, Saglam E, Uzbay IT (January 2006). "Discriminative stimulus properties of tianeptine". Psychopharmacology 183 (4): 446–51. doi:10.1007/s00213-005-0210-5. PMID 16292591.  
  12. ^ Charles Malen, Bernard Danrée, Jean-Claude Poignant. Nouveaux dérivés tricycliques et leur procédé de préparation. French Patent FR 2104728, 7th September 1971.







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