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CAS NO.66981-73-5
Tianeptine, a tricyclic compound, is a selective facilitator of 5-HT (serotonin; sc-201146) uptake in vitro and in vivo. Additionally, Tianeptine is reported to act as a selective inhibitor of dopamine uptake and is similar to amineptine. Tianeptine does not have a noted effect on monoamine uptake. In a study utilizing purified synaptosomes from rat brain, Tianeptine was reported to enhance serotonin uptake in selective brain regions. Purified synaptosomes were obtained from rats and incubated with tritium-labeled 5-H and Tianeptine in vitro . The synaptosomes were then analyzed for uptake and release of 5-HT via a liquid scintillation counter.
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.
Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo. Tianeptine 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.
| Item Name | Tianeptine acid |
| CAS NO | 66981-73-5 |
| Apparence | White Powder |
| Package | 1g.10g,50g,100g,1000g,2000g or 25000g |
| Function |
Tianeptine is a prescription medication used to treat depression in all its ranges of severity. The tianeptine medication is generally described as a tricyclic antidepressant. This is a chemical compound so named because it contains three rings of atoms. Like other tricyclic antidepressants, tianeptine blocks the reuptake, or re-absorption, of serotonin. This is a neurotransmitter responsible for one’s sense of well-being. The reuptake consequently increases the availability of such substances to the brain. |
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