Description Appearance biological activity Biochem/physiol Actions Laboratory Procedures
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Tianeptine sodium salt

Description Appearance biological activity Biochem/physiol Actions Laboratory Procedures
Product Name
Tianeptine sodium salt
CAS No.
30123-17-2
Chemical Name
Tianeptine sodium salt
Synonyms
TIANEPTINE SODIUM;Tianeptine Free Acid;Stablon;S-1574;99% purity 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;tianeptin sodium;Coaxil sodiuM salt;tianeptin-a sodium;Tianeptine Sodium SaL
CBNumber
CB9279090
Molecular Formula
C21H24ClN2NaO4S
Formula Weight
458.93
MOL File
30123-17-2.mol
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Tianeptine sodium salt Property

Melting point:
1800C
storage temp. 
Desiccate at RT
solubility 
DMSO: ≥20mg/mL
form 
solid
color 
white to tan
Merck 
14,9420
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 2 months.
InChIKey
ZLBSUOGMZDXYKE-UHFFFAOYSA-M
SMILES
C1(NCCCCCCC([O-])=O)C2C=CC=CC=2N(C)S(=O)(=O)C2C=C(Cl)C=CC1=2.[Na+]
CAS DataBase Reference
30123-17-2(CAS DataBase Reference)
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Safety

WGK Germany 
3
HS Code 
2934.99.4400
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H332Harmful if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P322Specific measures (see …on this label).

P330Rinse mouth.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
T1692
Product name
Tianeptine sodium salt hydrate
Purity
≥98% (HPLC), powder
Packaging
5mg
Price
$337
Updated
2024/03/01
Sigma-Aldrich
Product number
T1692
Product name
Tianeptine sodium salt hydrate
Purity
≥98% (HPLC), powder
Packaging
25mg
Price
$1220
Updated
2024/03/01
TCI Chemical
Product number
T3131
Product name
Tianeptine Sodium Salt Hydrate
Purity
>98.0%(HPLC)(N)
Packaging
200mg
Price
$139
Updated
2024/03/01
TCI Chemical
Product number
T3131
Product name
Tianeptine Sodium Salt Hydrate
Purity
>98.0%(HPLC)(N)
Packaging
1g
Price
$418
Updated
2024/03/01
Cayman Chemical
Product number
17561
Product name
Tianeptine (sodium salt)
Purity
≥95%
Packaging
50mg
Price
$32
Updated
2024/03/01
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Tianeptine sodium salt Chemical Properties,Usage,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.

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 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 .

Originator

Sci. Union et Cie (France)

Uses

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.

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

General Description

Tianeptine is a μ-opioid receptor (MOR) as well as a δ-opioid receptor (DOR) agonist.

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 .

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.

References

1)?Mennini?et al. (1987),?Tianeptine, a selective enhancer of serotonin uptake in rat brain; ?Naunyn-Schmied. Arch. Pharmacol.,?336?478 2)?Kato and Weitsch (1988),?Neurochemical profile of tianeptine, a new antidepressant drug; ?Clin. Neuropharmacol.,?11?S43 3)?Plaisant?et al. (2003),?Neuroprotective properties of tianeptine: interactions with cytokines; Neuropharmacology,?44?801 4)?Seo?et al. (2016),?Tianeptine induces mTORC1 activation in rat hippocampal neurons under toxic conditions; ?Psychopharmacology (Berl.),?233?2617 5)?Slusarczyk?et al. (2017),?Anti-inflammatory properties of tianeptine on lipopolysaccharide-induced changes in microglial cells involve toll-like receptor-related pathways; ?J. Neurochem.,?136?958

Tianeptine sodium salt Preparation Products And Raw materials

Raw materials

Preparation Products

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Tianeptine sodium salt Suppliers

Shandong kelikang drug co., ltd
Tel
0531-88113608
Email
kelikangpharm@163.com
Country
China
ProdList
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Jinan Jianfeng Chemical Co., Ltd.
Tel
0531-88110457 15562555968
Email
info@pharmachemm.com
Country
China
ProdList
166
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58
Shandong RuiYue Biotechnology Co., Ltd.
Tel
0531-88581623 18805314509
Fax
0531-88581623
Email
1456922171@126.com
Country
China
ProdList
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Shandong Mingfeng Pharmaceutical and Technology Co. Ltd
Tel
-1345456643 15315114555
Fax
QQ:1345456643
Email
1345456643@qq.com
Country
China
ProdList
248
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Hefei Chaobo Technology Co., Ltd
Tel
19322001459
Email
zb19922001456@163.com
Country
China
ProdList
471
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Wuhan Yida Pharmaceutical Co., Ltd
Tel
+86-13401188533 +86-13476102740
Email
3451936732@qq.com
Country
China
ProdList
64
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J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
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INTATRADE GmbH
Tel
+49 3493/605464
Fax
+49 3493/605470
Email
sales@intatrade.de
Country
Germany
ProdList
3576
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3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15848
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JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9984
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View Lastest Price from Tianeptine sodium salt manufacturers

Dorne Chemical Technology co. LTD
Product
Tianeptine sodium salt 30123-17-2
Price
US $10.00-10.00/ASSAYS
Min. Order
1ASSAYS
Purity
99%
Supply Ability
10 tons
Release date
2024-03-26
Wuhan Cell Pharmaceutical Co., Ltd
Product
Tianeptine sodium 30123-17-2
Price
US $3.20-290.00/g
Min. Order
1g
Purity
99%
Supply Ability
1000kg
Release date
2023-03-27
Hebei Kangcang new material Technology Co., LTD
Product
Tianeptine sodium salt 30123-17-2
Price
US $300.00-100.00/kg
Min. Order
1kg
Purity
99.99%
Supply Ability
100ton/ month
Release date
2024-03-08

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