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ID: 2781964
User: 79.138.33.214
Article: Tianeptine
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Updating {{infobox_drug}} (changes to verified and watched fields) per Chem/infobox_drug validation (report errors or bugs)
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Tianeptine has been found to be an efficacious [[μ-opioid receptor]] [[agonist]] ([[Ligand (biochemistry)#Receptor/ligand binding affinity|K<sub>i</sub>]] (human) of 383 ± 183 nM and EC<sub>50</sub> (human) of 194 ± 70 nM). The same study revealed that it is also a [[δ-opioid receptor]] agonist, although with much lower potency.<ref name = gassa>{{cite journal |author1=Gassaway, MM |author2=Rives, MLL |author3=Kruegel, AC |author4=Javitch, JA |author5=Sames, D |title=The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist.|journal=Translational Psychiatry|volume=4|date=July 2014|pmid=25026323|doi=10.1038/tp.2014.30|issue=7|url=http://www.nature.com/tp/journal/v4/n7/full/tp201430a.html|pages=e411}}</ref> These actions are responsible for the [[abuse potential]] of the drug at high doses well above the normal therapeutic range.
Tianeptine has been found to be an efficacious [[μ-opioid receptor]] [[agonist]] ([[Ligand (biochemistry)#Receptor/ligand binding affinity|K<sub>i</sub>]] (human) of 383 ± 183 nM and EC<sub>50</sub> (human) of 194 ± 70 nM). The same study revealed that it is also a [[δ-opioid receptor]] agonist, although with much lower potency.<ref name = gassa>{{cite journal |author1=Gassaway, MM |author2=Rives, MLL |author3=Kruegel, AC |author4=Javitch, JA |author5=Sames, D |title=The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist.|journal=Translational Psychiatry|volume=4|date=July 2014|pmid=25026323|doi=10.1038/tp.2014.30|issue=7|url=http://www.nature.com/tp/journal/v4/n7/full/tp201430a.html|pages=e411}}</ref> These actions are responsible for the [[abuse potential]] of the drug at high doses well above the normal therapeutic range.


{| class="wikitable"
|+'''Binding profile'''<ref name=mp09/><ref name=CNS2008 /><ref name = gassa/>
|-
! Protein !! K<sub>i</sub> (nM) for tianeptine !!
|-
| [[Serotonin transporter|SERT]] || ?
|-
| [[Delta opioid receptor|δ<sub>1</sub> opioid receptor]] || 37.4 ± 11.2 μM (0.0374 nM)
|-
| [[Kappa opioid receptor|κ<sub>1</sub> opioid receptor]] || Inactive
|-
| [[Mu opioid receptor|μ opioid receptor]] || 383 ± 183
|-
| [[NMDA receptor| NMDA receptor]] || ?
|-
| [[AMPA receptor| AMPA receptor]] || ?
|}


==Development==
==Development==
Reason: ANN scored at 0.929111
Reporter Information
Reporter: Mind_paralysis (anonymous)
Date: Tuesday, the 7th of July 2020 at 01:15:39 PM
Status: Reviewed - Not included in dataset
Monday, the 3rd of October 2016 at 10:01:47 AM #106205
Mind_paralysis (anonymous)

Added table showing different sites of binding for Tianeptine - NOT, I repeat, NOT an attempt at vandalism.