|Name||Tianeptine sodium salt|
|Synonyms||Sodium 7-((3-chloro-6,11-dihydro-6-methyldibenzo(c,f)(1,2)thiazepin-11-yl)amino)heptanoate S,S-dioxide|
|CAS Registry Number||30123-17-2 (54317-11-2)|
|Density || 1.38|
|Melting Point || 180℃|
|Boiling Point || 609.2 °C at 760 mmHg|
|Flash Point || 322.2 °C|
|Appearance || solid|
|Solubility || DMSO: ≥20mg/mL|
Tianeptine sodium salt is a salt of Tianeptine. Tianeptine 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.5It also reverses increases in extracellular glutamate levels induced by acute restraint stress in the basolateral nucleus of the amygdala in rats.
It is used to treat mild, moderate or severe depression, neurogenic and reactive depression, anxiety and depression of body, especially gastrointestinal discomfort, and anxiety and depression of alcohol-dependent patients during withdrawal. The recommended dose is 12.5mg, TID, orally before morning, afternoon and evening main meals. Dose adjustment is not required for chronic alcoholics, regardless of liver cirrhosis. The dose is limited to 2 tablets per day for patients over 70 years of age and with renal insufficiency.
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