Tianeptine Sodium powder (30123-17-2)

Tianeptine powder is an atypical antidepressant. 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. 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. 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. 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. It also reverses increases in extracellular glutamate levels induced by acute restraint stress in the basolateral nucleus of the amygdala in rats.

Tianeptine sodium powder is a selective enhancer of serotonin uptake in the brain with no effect on noradrenalin or dopamine uptake. Clinically useful antidepressant. Displays neuroprotective effects against hypoxia in cell culture and against the deleterious effects of cytokines in vivo. Induces mTORC1 activation in rat hippocampal neurons and increases dendritic outgrowth, spine density and synaptic proteins. Attenuates LPS-evoked inflammatory activation of microglial cells in culture.

Selective facilitator of 5-HT uptake in vitro and in vivo. Has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant, analgesic and neuroprotective following systemic administration in vivo.

Tianeptine (trade names Stablon and Coaxil) is a pharmaceutical compound most commonly used for the treatment of clinical depression. It is also sometimes used to treat irritable bowel syndrome or asthma. At heavy doses it is reported to produce opioid-like recreational effects such as sedation and stimulation, motivation enhancement, and euphoria when administered.

In terms of chemical classification, tianeptine is a tricyclic antidepressant (TCA). However, its pharmacology and effects vary from those of typical antidepressant and anxiolytics, mainly in the fact that it is not thought to act immediately through the regulation of monoaminergic neurotransmitters (such as serotonin, dopamine, and noradrenaline.) Rather, tianeptine is theorized to act upon glutamate and glutamatergic mechanisms, causing the brain to adapt more readily to stress and depression.

Sodium has been assayed as a steatosis-positive inducer in HepG2 cells. Tianeptine has also been used to study effects on rats exposed to swim endurance tests (SETs). This study reported that tianeptine increased swimming time in rats undergoing SET. Moreover, tianeptine also increased total cholesterol and LDL, while triglyceride levels were decreased. Thus, tianeptine may be involved in the pathogenesis of metabolic syndrome.

Tianeptine sodium is a water-soluble tricyclic antidepressant agent. In contrast with classical tricyclic antidepressants or selective serotonin reuptake inhibitors (SSRIs), tianeptine is a selective serotonin reuptake enhancer (SSRE) in brain and reduces stress-induced atrophy of neuronal dendrites. (The product is for research purpose only.)Clinical trials of tianeptine suggest it is just as effective as other more popular antidepressants such as fluoxetine (a SSRI) and amitriptyline (a TCA). However, Tianeptine seems to exhibit fewer side effects and complications than traditional antidepressants.

In addition to its antidepressant effects, tianeptine also exhibits anxiolytic (anti-anxiety) properties, specifically showing promise in the treatment of panic disorders. Tianeptine also displays neuroprotective properties and improves cognition in patients with depression. Tianeptine’s anxiolytic and mood-boosting effects, in addition to its neuroprotective and cognitive benefits, make it a popular nootropic.

Prescription guidelines indicate that tianeptine should be taken in 12.5 mg doses and taken three times daily, waiting 3-4 hours between doses.

COA

• Mennini, T., et al. 1987. Naunyn Schmiedebergs Arch. Pharmacol. 336: 478-482. PMID: 3437921
• The Most Strong Antidepressant: Tianeptine Sodium In 2019