Tianeptine sodium salt
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Tianeptine sodium salt
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CAS No:
30123-17-2
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Formula:
C21H24ClN2NaO4S
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Chemical Name:
Tianeptine sodium salt
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Synonyms:
TIANEPTINE SODIUM;TIANEPTINE SODIUM SALT;7-[(3-Chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic Acid S,S-Dioxide Sodium Salt;S-1574;Stablon;7-[(3-chloro-6,11-dihydro-6-methyl-dibenzo[c,f][1,2]thiazepine-11-yl)amino]heptanoic acid s,s dioxide sodium salt;[7-[(3-Chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepine 5,5-dioxide)-11-ylamino]heptanoic acid]sodium salt;3-Chloro-6,11-dihydro-6-methyl-11-[6-(sodiooxycarbonyl)hexylamino]dibenzo[c,f][1,2]thiazepine 5,5-dioxide
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CAS No:
Description
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.
Tianeptine sodium salt is a structurally novel, serotonin specific antidepressant. It is useful in the treatment of neurotic and reactive depressions, as well as depressive states accompanied by anxiety. Tianeptine (sodium salt) is an analytical reference standard categorized as an opioid. Tianeptine has been abused and associated with overdose and death. Formulations containing tianeptine have been used in the treatment of depression. This product is intended for use in analytical forensic applications. This product is also available as a general research tool .
Tianeptine is a μ-opioid receptor (MOR) as well as a δ-opioid receptor (DOR) agonist.
Tianeptine sodium salt Use and Manufacturing
Tianeptine sodium salt is a tricyclic compound with psychostimulant, anti-ulcer and anti-emetic properties. Tianeptine sodium salt hydrate has been used as a selective serotonin reuptake enhancer (SSRE) positive control during serotonin transporter (SERT) assay in human embryonic kidney 293 cell lines. Tianeptine (INN) (Stablon, Coaxil, Tatinol) is a SSRE drug used for treating major depressive episodes (mild, moderate, or severe). Tianeptine commonly used for depression. It is also used for pain, asthma, anxiety, and many other conditions, but there is no good scientific evidence to support these other uses.
Drug Function and Efficacy
Antidepressants increase the spontaneous activity of pyramidal cells in the hippocampus, accelerate recovery after functional inhibition, and speed up the uptake of serotonin by neurons in the cerebral cortex and hippocampus; their effects on the human body are between those of sedative and stimulant antidepressants, significantly improving symptoms of physical discomfort, especially gastrointestinal discomfort symptoms related to anxiety and mood disorders; and relieving personality and behavioral abnormalities that occur in alcohol-dependent patients during withdrawal.
Registered Holders
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QUIMICA SINTETICA SA
Active
Spain
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Servier (Tianjin) Pharmaceutical Co., Ltd.
Active
China
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QUIMICA SINTETICA S.A.
Active
European Union
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