Introduction to Tianeptine Sodium Salt

Tianeptine sodium salt, also known as Datilang; Sulfamethoxazole; and Thionaproxen is a novel tricyclic antidepressant that exerts antidepressant effects by acting on the 5-HT system. It is mainly used clinically to treat depression. Tianeptine sodium salt has a good effect on mood disorders and has a significant effect on physical discomfort symptoms, especially gastrointestinal discomfort symptoms related to anxiety and mood disorders. In animal experiments, it has been observed that Tianeptine sodium salt can increase the spontaneous activity of pyramidal cells in the hippocampus, accelerate the recovery after functional inhibition, and accelerate the uptake of serotonin by neurons in the cerebral cortex and hippocampus.

Figure 1 Characteristics of Tianeptine sodium salt

Pharmacological effects of Tianeptine sodium salt

Tianeptine sodium salt is a tricyclic antidepressant drug, and its antidepressant mechanism is different from traditional tricyclic antidepressants. It can increase the reuptake of 5-HT in the synaptic cleft and may affect enhancing 5-HT neuronal conduction. Has no affinity for cholinergic or adrenergic receptors. The antidepressant efficacy is similar to tricyclic drugs, but the tolerability is better than tricyclic drugs. In animal experiments, it can increase the spontaneous activity of pyramidal cells in the hippocampus and accelerate their recovery after functional inhibition; Can increase the reabsorption of serotonin by neurons in the cerebral cortex and hippocampus. Thiamethasone sodium is rapidly and completely absorbed in the digestive tract. The distribution is rapid, with a PPB of up to 94%. In the liver, complete metabolism is achieved through β - oxidation and N-demethylation, and the clearance of terminal T1/2 is short, taking 2.5 hours. A very small amount of the original drug (8%) is excreted from the kidneys, mainly its metabolites are excreted from the urine. The clearance of T1/2 in patients with renal insufficiency is prolonged by 1 hour.

Application of Tianeptine Sodium Salt

Tianeptine sodium salt is mainly used in medical research and drug development. It is mainly used in clinical practice in the form of Tenotentine sodium to treat the following diseases.

Depression: often applicable to patients with chronic depression and depression accompanied by anxiety.

Anxiety disorder: By regulating the stress response system, it helps alleviate anxiety symptoms.

Chronic pain: It exhibits potential adjuvant therapeutic effects in conditions such as fibromyalgia.

In addition, Tianeptine sodium salt is widely used in neuroscience research to explore mechanisms related to stress, depression, and neurology.

In vivo study of Tianeptine Sodium Salt

In non stress rats, Tianeptine sodium salt treatment prevented an increase in corticotropin releasing factor (CRF) mRNA levels induced by CMS in dBNST and reduced CRF mRNA levels in dBNST. Tianeptine sodium salt treatment significantly reduced CRF mRNA levels of ventral BNST and CEA in the stress avoidance control group and CMS exposed rats. In the basal lateral nucleus (BLA) of the amygdala in anesthetized rats, Tianeptine sodium salt blocks stress-induced PB enhancement in the CA1 region without affecting stress-induced enhancement of LTP. Tianeptine sodium salt was administered with enhanced PB enhancement under non stress conditions in the amygdala, hippocampus, and LTP of anesthetized rats. In rats, Tianeptine sodium salt attenuates peripheral induction rather than central, LPS, or IL-1 β - induced pathological behavior. In rats, Tianeptine sodium salt normalized the amplitude ratio of AMPA/kainate receptor-mediated currents to NMDA receptors and prevented stress-induced NMD-EPSCS inactivation. Both in control and stressed animals, Tianeptine sodium salt significantly reduced cell apoptosis in the temporal cortex and dentate gyrus of rats, but had no effect on Anmeng in the Horn of Africa. Only in the nucleus accumbens, Tianeptine sodium salt (2.5 mg/kg, intraperitoneal injection) increased extracellular dopamine. Tianeptine sodium salt significantly increased the extracellular concentrations of hydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in both the striatum and striatum.

Reference

[1] El-Setouhy D A, El-Malak N S A. Formulation of a novel tianeptine sodium orodispersible film[J]. Aaps Pharmscitech, 2010, 11: 1018-1025.

[2] Jayasooriya R G P T, Dilshara M G, Choi Y H, et al. Tianeptine sodium salt suppresses TNF-α-induced expression of matrix metalloproteinase-9 in human carcinoma cells via suppression of the PI3K/Akt-mediated NF-κB pathway[J]. Environmental Toxicology and Pharmacology, 2014, 38(2): 502-509.