Tianeptine sodium salt

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Cat Number

API30123172

CAS Number

30123-17-2

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Product Detail Description Scientific Support Customer Q&A

CAS Number

30123-17-2

EINECS

250-059-3

Storage

Room temperature

Synonyms

7-[(3-Chloro-6,11-dihydro-6-methyldibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic Acid S,S-Dioxide Sodium Salt

Molecular Formula

C21H24ClN2NaO4S

Molecular Weight

458.93

Smiles

C1(NCCCCCCC([O-])=O)C2C=CC=CC=2N(C)S(=O)(=O)C2C=C(Cl)C=CC1=2.[Na+]

Appearance

White to tan solid

Melting Point

1800℃

Relative Density

1.38

General Description

Tianeptine sodium salt is an atypical tricyclic antidepressant and a Selective Serotonin Reuptake Enhancer (SSRE). It is rapidly and completely absorbed in the gut and distributed in the body. In terms of its antidepressant properties it is similar to classical tricyclic antidepressants but it is better tolerated and has a much better side-effect profile.

Mechanism of Action

Tianeptine sodium salt's main action is the enhancement of serotonin (5-HT) reuptake into the presynaptic nerve ending, in direct contrast to the SSRIs. This is thought to normalise serotonergic neurotransmission. Tianeptine is a moderate μ-opioid receptor agonist and a weak δ-opioid receptor agonist. It is a glutamate modulator, potentiating AMPA receptor activity and antagonising the NMDA receptor.

Application

Tianeptine sodium salt is indicated in the treatment of a spectrum of depressive disorders, including major depressive episodes and neurogenic or reactive depression. It has been effectively used in the treatment of anxiety-depressive states with marked somatic symptoms such as anxiety-depressive gastrointestinal disorders and in the reduction of anxiety-depressive symptoms in alcohol-dependent patients. It is also used in research on pain reduction.

Tianeptine is a non-monoaminergic atypical antidepressant. It does not block serotonin, norepinephrine or dopamine re-uptake, bind to >100 classic receptors or inhibit MAO. Instead, it is a weak but functionally effective Mu- and Delta-opioid receptor agonist, that increases limbic dopamine, prevents morphine tolerance and has anti-inflammatory effects on microglia without opioid dependence.
Tianeptine regulates glutamate by normalising stress-induced overflow, up-regulating glial transporters, antagonising glycine-B site of NMDA receptors, and potentiating AMPA receptors to restore synaptic plasticity. Chronic treatment up-regulates BDNF, NGF and CREB, reverses dendritic atrophy, stimulates hippocampal neurogenesis and normalises mitochondrial respiratory-chain deficits/oxidative stress. It also normalises hyperactive HPA axis by decreasing ACTH/corticosterone and restoring glucocorticoid receptor sensitivity. These multiple actions combine to produce rapid antidepressant and anxiolytic effects, along with improving somatic and cognitive symptoms, with efficacy in SSRI-resistant, parkinsonian or PTSD depression without sedation or cardiovascular liability.
In conclusion, Tianeptine is a glutamate- and neuroplasticity-focused approach that can complement monoaminergic antidepressants.

Fig. 1 Mechanism of action of Tianeptine in treating antidepressant. (Alamo C.; et al. 2019)

References

Alamo C, et al. Tianeptine, an atypical pharmacological approach to depression. Revista de Psiquiatría y Salud Mental (English Edition), 2019, 12(3): 170-186.

How should Tianeptine sodium salt be stored?

Store at room temperature (RT).

What is the main mechanism of action of Tianeptine sodium salt?

It functions as a Selective Serotonin Reuptake Enhancer (SSRE) and modulates glutamate and opioid receptors.

What are the primary applications of Tianeptine sodium salt?

It is used for treating depressive disorders, anxiety-depressive states, and in pain research.

Do you ship Tianeptine sodium salt globally?

Yes, we serve major countries and regions worldwide.