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Tianeptine sodium salt

Description Appearance biological activity Biochem/physiol Actions Uses Laboratory Procedures
Tianeptine sodium salt
Tianeptine sodium salt structure
CAS No.
30123-17-2
Chemical Name:
Tianeptine sodium salt
Synonyms
S-1574;Stablon;tianeptin sodium;TIANEPTINE SODIUM;Coaxil sodiuM salt;tianeptin-a sodium;Tianeptine Free Acid;Tianeptine Sodium SaL;Tianeptin Sodium Salt;TIANEPTINE SODIUM SALT
CBNumber:
CB9279090
Molecular Formula:
C21H24ClN2NaO4S
Formula Weight:
458.93
MOL File:
30123-17-2.mol

Tianeptine sodium salt Properties

Melting point:
1800C
storage temp. 
Desiccate at RT
solubility 
DMSO: ≥20mg/mL
form 
solid
color 
white to tan
Merck 
14,9420
InChIKey
ZLBSUOGMZDXYKE-UHFFFAOYSA-M
CAS DataBase Reference
30123-17-2(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
WGK Germany  3

Tianeptine sodium salt price More Price(10)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich T1692 Tianeptine sodium salt hydrate ≥98% (HPLC), powder 30123-17-2 5mg $282 2021-03-22 Buy
Sigma-Aldrich T1692 Tianeptine sodium salt hydrate ≥98% (HPLC), powder 30123-17-2 25mg $1020 2021-03-22 Buy
TCI Chemical T3131 Tianeptine Sodium Salt Hydrate >98.0%(HPLC)(N) 30123-17-2 200mg $142 2021-03-22 Buy
TCI Chemical T3131 Tianeptine Sodium Salt Hydrate >98.0%(HPLC)(N) 30123-17-2 1g $493 2021-03-22 Buy
Cayman Chemical 17561 Tianeptine (sodium salt) ≥95% 30123-17-2 1g $275 2021-03-22 Buy

Tianeptine sodium salt Chemical Properties,Uses,Production

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.

Appearance

White to pale yellow solid.

biological activity

Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo. IC50 Value:Target: 5-HT ReceptorTianeptine 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.

Biochem/physiol Actions

Tianeptine is a tricyclic antidepressant that enhances serotonin uptake. This drug can affect neuroprotection, neuronal excitability, memory and anxiety. However, tianeptine is not linked to adverse psychomotor, cognitive, cardiovascular, sleep and bodyweight effects. The drug has a low tendency for abuse and has a positive pharmacokinetic profile.
Tianeptine is least involved in drug interaction as it is not metabolized by cytochrome P450 system in the liver. In hippocampus and amygdala, tianeptine is involved in glutamatergic transmission processes and elicits neuroplasticity.

Uses

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.

Laboratory Procedures

Tianeptine (sodium salt) is supplied as a crystalline solid. A stock solution may be made by dissolving the tianeptine (sodium salt) in the solvent of choice. Tianeptine (sodium salt) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of tianeptine (sodium salt) in these solvents is approximately 10, 20, and 30 mg/ml, respectively. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of tianeptine (sodium salt) can be prepared by directly dissolving the crystalline solid in aqueous buffers. The solubility of tianeptine (sodium salt) in PBS, pH 7.2, is approximately 10 mg/ml. We do not recommend storing the aqueous solution for more than one day.

Description

Tianeptine sodium 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.

Chemical Properties

White to Yellowish Powder

Originator

Sci. Union et Cie (France)

Uses

Tricyclic compound with psychostimulant, anti-ulcer and anti-emetic properties. Antidepressant

Uses

Tianeptine (INN) (Stablon, Coaxil, Tatinol) is a selective serotonin reuptake enhancer (SSRE) drug used for treating major depressive episodes (mild, moderate, or severe). Unlike conventional tricyclic antidepressants, tianeptine enhances the reuptake of

Manufacturing Process

A solution of 27.6 g (0.16 mol) of freshly distilled ethyl 7-aminoheptanoate in 40 ml of nitromethane was added all at once and with mechanical stirring to a suspension of 26.2 g (0.08 mol) of 5,8-dichloro-10-dioxo-11- methyldibenzo[c,f]thiazepine(1,2) in 120 ml of nitromethane. The whole was heated to 55°C for 30 minutes, the solvent was then evaporated in vacuo and the residue was taken up in water. The crude ester was extracted with ether. After evaporation of the ether 36 g of crude ester were obtained, and 30 g (0.065 mol) there of were treated under reflux with a solution of 2.8 g (0.07 mol) of sodium hydroxide in 35 ml of ethanol and 25 ml of water. After one hour's refluxing, the alcohol was evaporated in vacuo. The residue was taken up in 150 ml of water.
The mixture was twice extracted with 75 ml of chloroform and the aqueous phase was evaporated in vacuo. The sodium salt was then dissolved in 150 ml of chloroform, the solution was dried over sodium sulfate and the product precipitated with anhydrous ether.
The salt was filtered off, washed with ether and dried at 50°C. 13 g of sodium 7-[8-chloro-10-dioxo-11-methyldibenzo[c,f]thiazepin-(1,2)-aminoheptanoate,melting with decomposition at about 180°C, were obtained.

brand name

STABLON

Therapeutic Function

Antidepressant

Biological Activity

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 (IC 50 > 10 μ M) and has no effect on noradrenalin or dopamine uptake. Antidepressant, analgesic and neuroprotective following systemic administration in vivo .

Tianeptine sodium salt Preparation Products And Raw materials

Raw materials

Preparation Products


Tianeptine sodium salt Suppliers

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Jinan Jianfeng Chemical Co., Ltd
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XI'AN TIANGUANGYUAN BIOTECH CO., LTD.
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View Lastest Price from Tianeptine sodium salt manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-10-22 Tianeptine sodium salt
30123-17-2
US $60.00 / KG 1KG 99% 10 tons Hanhong Medicine Technology (Hubei) Co., Ltd.
2021-10-22 Tianeptine sodium salt
30123-17-2
US $1.00 / ASSAYS 1ASSAYS 99% 20 tons Jinan Jianfeng Chemical Co., Ltd
2021-10-22 Tianeptine sodium
30123-17-2
US $1.00 / KG 1KG 99 100Kg Jinan Ande Pharmaceutical Co.,Ltd.

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