Tianeptine sodium

Tianeptine sodium (CAS No.: 30123-17-2) is an atypical antidepressant and neuropsychopharmacological agent widely utilized in biomedical research to investigate mood regulation, stress response, and neuroplasticity. Unlike classical monoaminergic antidepressants, it functions as a selective facilitator of serotonin (5-HT) uptake in vitro and in vivo while exhibiting negligible affinity for a broad range of neurotransmitter receptors, including serotoninergic and dopaminergic systems, at concentrations in the micromolar range, and does not significantly alter noradrenaline or dopamine uptake. Mechanistically, tianeptine sodium acts as a moderate agonist of the μ-opioid receptor and, to a lesser extent, the δ-opioid receptor, and also modulates glutamatergic neurotransmission through enhancement of AMPA receptor activity and inhibition of NMDA receptor signaling. It further influences adrenergic signaling by increasing α1 receptor sensitivity following chronic exposure. In cellular and animal models, tianeptine sodium demonstrates neuroprotective properties under stress- and inflammation-related conditions, partly through anti-inflammatory and antioxidant effects and suppression of MMP-9 via inhibition of the PI3K/Akt-mediated NF-κB pathway. These pharmacological characteristics make it a valuable tool for studying synaptic plasticity, neuroinflammation, and mood disorder pathophysiology, as well as for screening compounds targeting opioid and glutamatergic pathways, with experimental concentrations or dosing regimens varying according to specific assay designs and research objectives.