Hot Products
High Purity Tianeptine 99% | CAS 66981-73-5 | Trusted China Suppliers & Factory for Safe Delivery
Description
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.
Uses
Tianeptine is used in the treatment of reactive and neurotic depression, as well as in the treatment of anxious states. It is a tricyclic compound with psychostimulant, anti-ulcer and anti-emetic properties.
Tianeptine is a drug used primarily in the treatment of major depressive disorder, although it may also be used to treat asthma or irritable bowel syndrome. Chemically it is a tricyclic antidepressant (TCA), but it has different pharmacological properties than typical TCAs as recent research suggests that tianeptine produces its antidepressant effects through indirect alteration of glutamate receptor activity (i.e., AMPA receptors and NMDA receptors) and release of BDNF, in turn affecting neural plasticity.
Definition
Tianeptine is a racemate comprising of equimolar amounts of (R)- and (S)-tianeptine. It is an atypical antidepressant used in Europe to treat patients who respond poorly to selective serotonin reuptake inhibitors (SSRIs). It has a role as a mu-opioid receptor agonist, a second generation antipsychotic and an anxiolytic drug. It contains a (R)-tianeptine and a (S)-tianeptine.
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.
Details
Frequently Asked Questions
What is Tianeptine primarily used for?
Tianeptine is mainly used to treat major depressive disorder, reactive and neurotic depression, and various anxious states.
How does Tianeptine differ from typical tricyclic antidepressants?
Unlike typical TCAs, Tianeptine works by indirectly altering glutamate receptor activity (AMPA and NMDA) and releasing BDNF, which affects neural plasticity.
Can Tianeptine be used for physical conditions?
Yes, research indicates it may also be used in the treatment of asthma and irritable bowel syndrome (IBS).
What are the pharmacological roles of Tianeptine?
It acts as a mu-opioid receptor agonist, an atypical antidepressant, an anxiolytic drug, and a second-generation antipsychotic.
What is the chemical composition of Tianeptine?
Tianeptine is a racemate consisting of equal amounts of (R)- and (S)-tianeptine enantiomers.
Does Tianeptine affect serotonin levels?
Yes, it is a selective facilitator of 5-HT (serotonin) uptake in both in vitro and in vivo environments.