An atypical antidepressant; an agonist of MORs (EC50s = 194 and 641 nM for human and mouse receptors in a BRET assay for G protein activation; decreases immobility in the forced swim test in wild-type

Tianeptine (sodium salt) – 500 mg

Brand:
Cayman
CAS:
30123-17-2
Storage:
-20
UN-No:
Non-Hazardous - /

Tianeptine is an atypical antidepressant.{28646} It is an agonist of the μ-opioid receptor (MOR; EC50s = 194 and 641 nM for human and mouse receptors, respectively, in a BRET assay for G protein activation) and also has effects on the glutamate system.{28646,28645} Tianeptine (30 mg/kg) decreases immobility in the forced swim test in wild-type, but not MOR knockout mice, indicating antidepressant-like activity dependent on MORs.{43567} It increases locomotor activity at a dose of 30, but not 10 mg/kg, in the open field test and increases paw withdrawal latency in the hot-plate test in mice. Tianeptine modulates AMPA receptor activity by increasing phosphorylation of the AMPA receptor GluR1 subunit in the frontal cortex and hippocampal CA3 region in mice.{43568} It prevents increases in glial glutamate transporter 1 (GLT-1) expression induced by chronic restraint stress in the hippocampal CA3 region in rats when administered at a dose of 10 mg/kg per day for 21 days.{43569} It also reverses increases in extracellular glutamate levels induced by acute restraint stress in the basolateral nucleus of the amygdala in rats.{43570}  

 

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Description

An atypical antidepressant; an agonist of MORs (EC50s = 194 and 641 nM for human and mouse receptors in a BRET assay for G protein activation; decreases immobility in the forced swim test in wild-type, but not MOR knockout mice at 30 mg/kg; increases locomotor activity at a dose of 30, but not 10 mg/kg, in the open field test; prevents increases in chronic restraint stress-induced GLT-1 expression in the rat hippocampal CA3 region at 10 mg/kg per day for 21 days

Formal name: 7-[(3-chloro-6,11-dihydro-6-methyl-5,5-dioxidodibenzo[c,f][1,2]thiazepin-11-yl)amino]-heptanoic acid, monosodium salt

Synonyms: 

Molecular weight: 458.9

CAS: 30123-17-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Depression

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