Description

Tianeptine sodium salt, also known as Stablon or Coaxil, usually appears as a white or slightly yellow crystalline powder. It is similar in appearance to other powdery solids, although tiny grains or depressions may appear on the surface. The solubility in water is low. It is soluble in some organic solvents such as ethanol, ether and chloroform. However, its solubility in silver nitrate, mercury nitrate and cerium chloride is high. Considered a surfactant, it reduces the surface tension of liquids. Reducing surface tension, the cohesive force between the surface layer of a liquid and the molecules inside, makes it easier for the liquid to spread and transfer. is a drug with antidepressant and anxiolytic properties and its chemical name is 7-hydroxy-5,6,7,8-tetrahydronaphtho[1,2-a]pyridin-9-one. This article will focus on the physical properties of Tianeptine.

Chemical Formula

C21H24ClN2NaO4S-

Exact Mass

458

Molecular Weight

459

m/z

458 (100.0%), 460 (32.0%), 459 (22.7%), 461

Elemental Analysis

C, 54.96; H, 5.27; Cl, 7.72; N, 6.10; O, 13.94; S, Na, 5.01

The invention relates to a synthesis process of the drug Tianeptine sodium salt, in particular to a method for synthesizing thieneptine sodium by using 3-chloro-6-methyldibenzo [c, f] [1,2] thiazazol-11 (6H) – keto-5,5 – dioxide as the starting material, forming a Schiff base with amine, reducing, hydrolyzing and finally freeze-drying to salt. The starting material of the method is stable, easy to purchase, and the process is simple. The overall reaction conditions of the synthesis route are mild, the experimental operation is simple, and it is easy to realize industrial production.

In non stressed rats, the treatment of Tianeptine can prevent the increase of the mRNA level of corticotropin releasing factor (CRF) in dBNST induced by CMS, and reduce the mRNA level of corticotropin releasing factor (CRF) in dBNST. In the pressure avoidance control group and CMS exposed rats, Tianeptine treatment significantly reduced the level of CRF mRNA of ventral BNST and CEA. In the basolateral nucleus (BLA) of the amygdala in anesthetized rats, Tianeptine blocked the stress induced enhancement of PB in the CA1 region, but did not affect the stress induced enhancement of LTP. In the amygdala, hippocampus and LTP of anesthetized rats, Tianeptine was enhanced by administration of enhanced PB under non stress conditions.

In rats, Tianeptine attenuates peripheral induction rather than central, LPS or IL-1 β Behavioral signs of induced morbid behavior. In rats, Tianeptine caused the normalized proportion of AMPA/kainate receptor mediated current amplitude ratio from NMDA receptor and prevented the attenuation of stress induced inactivation of NMDA-EPSCS. In both control and stressed animals, in the temporal cortex and dentate gyrus of the rat, Tianeptine significantly reduced cell apoptosis, but had no effect on Amons in the Horn of Africa. In the nucleus accumbens only, Tianeptine (2.5 mg/kg, intraperitoneal injection) increases extracellular dopamine. In the two nucleus accumbens and striatum, Tianeptine significantly increased the extracellular concentrations of hydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA).

The following is a common laboratory synthesis method for Tianeptine sodium salt:

Preparation of raw materials:

01

O-Nitrochlorobenzene

O-nitrochlorobenzene is a common organic synthesis raw material that can be obtained through purchase or chemical synthesis methods. The structural formula of o-nitrochlorobenzene is C6H4ClNO2, with a molecular weight of 153.5.

02

Triethylamine

Triethylamine is an organic base with strong hygroscopicity. It can be prepared through the reaction of ethyl acetate and ammonia, or it can be purchased directly. The structural formula of triethylamine is (CH3CH2) 3N, with a molecular weight of 101.1.

03

Sodium acetate

Sodium acetate is an organic salt that is easily soluble in water and can be prepared by reacting acetic acid with sodium hydroxide, or directly purchased. The structural formula of sodium acetate is CH3COONa, with a molecular weight of 134.9.

04

Water

Water is the most common solvent in the laboratory and can be used to dissolve raw materials and products.

Synthesis steps:

product-1-1

Mix o-nitrochlorobenzene, triethylamine, and water together, heat to reflux state, and the reaction time is about 30 minutes to 1 hour.

After the reaction is completed, add sodium acetate and water, and then heat until dissolved.

Cool the solution to precipitate crystals. Stir with a glass rod and filter the crystals.

Wash the crystal to remove any residual mother liquor. Then dry the crystal to obtain the crude Tianeptine product.

Add the crude Tianeptine to an appropriate amount of water and heat it to a dissolved state. Add an appropriate amount of sodium hydroxide solution to adjust the pH value to around 7, then add an appropriate amount of activated carbon, heat and boil for a few minutes.

Filter and remove activated carbon particles, cool the solution, and precipitate crystals. Stir with a glass rod and filter the crystals to obtain Tianeptine high-quality products.

Wash and dry the Tianepine boutique to obtain the final product Tianepine sodium salt.

Tenepptin sodium salt is a tricyclic antidepressant. Its antidepressant mechanism is different from that of traditional tricyclic antidepressants. It can increase the reuptake of 5-HT in the synaptic space, which may have the effect of improving the conduction of 5-HT neurons. No affinity for choline or adrenaline receptors.

The antidepressant effect is similar to that of tricyclic drugs, but the tolerance is better than that of tricyclic drugs. In animal experiments, it can increase the spontaneous activity of pyramidal cells in the hippocampus and accelerate the recovery of their function after inhibition; It can increase the reabsorption of serotonin by neurons in cerebral cortex and hippocampus. Thioneptin sodium is absorbed rapidly and completely in the digestive tract. The distribution is rapid, and the PPB is up to 94%.

Through the liver β- The metabolism of oxidation and N-demethylation is complete, and the clearance terminal T1/2 is short, which is 2.5h. A small amount of prototype drug (8%) is excreted from the kidney, mainly its metabolite is excreted from the urine. T1/2 clearance was prolonged for 1 hour in patients with renal insufficiency.

Tianeptine sodium salt, also known as aminopeptidin or sodium aminopeptidin, is an organic compound with a molecular formula of C19H16N4Na2O4 and a molecular weight of 408.34. The following are the main uses of the product.

01

Antidepressants

Tianepine sodium salt is a drug with antidepressant activity that is widely used to treat various types of depression, including mild to severe depression. It works by regulating the levels of neurotransmitters serotonin (5-HT) and norepinephrine (NE) in the brain. Compared with traditional antidepressants, it has different mechanisms of action and pharmacological characteristics, making it an effective antidepressant.

02

Antianxiety drugs

Tianepine sodium salt is also used to treat anxiety disorders and stress reactions. It alleviates anxiety and stress responses by increasing the levels of serotonin and norepinephrine in the brain, while also affecting dopamine (DA) and γ- The aminobutyric acid (GABA) system also has a certain regulatory effect. This makes it a drug with anti anxiety activity and widely used to treat various types of anxiety disorders.

03

Improve memory and cognitive function

Research has found that Tianepine sodium salt has a certain impact on neurotransmitters in the brain, which can improve memory and cognitive function. It promotes neuronal excitability and plasticity by increasing the levels of dopamine and norepinephrine in the brain, and improves performance in areas such as attention, reaction time, and emotional management. These effects can be applied to treat neurocognitive disorders such as attention deficit hyperactivity disorder (ADHD).

04

Antifatigue drugs

Tianepine sodium salt is used as an anti-fatigue drug to alleviate physical fatigue and fatigue related symptoms. It improves the body’s fatigue and emotional state by regulating the levels of neurotransmitters serotonin and norepinephrine and increasing the release of dopamine. These effects can be applied to treat fatigue related diseases such as chronic fatigue syndrome.

05

Neuroprotective agents

Tianepine sodium salt has neuroprotective effects and can protect the brain from various neurodegenerative diseases and brain damage. It exerts neuroprotective effects by regulating the levels of neurotransmitters serotonin and norepinephrine and increasing the release of brain derived neurotrophic factor (BDNF). These effects can be applied to treat neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease.

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