Drug intelligence / Profile preview

tianeptine

Development stage
Phase 4
Lead developer
Servier
Modality
Small Molecules
Administration
Oral, Intravenous, Intranasal, Intramuscular, Rectal
01

Overview

Tianeptine is an atypical tricyclic antidepressant developed in the 1980s and used primarily for the treatment of major depressive disorder and anxiety in some European, Asian, and South American countries[1][2][5]. It is not approved for medical use in the United States but is sometimes sold as a dietary supplement or under various street names such as "gas station heroin"[2][3]. At low doses it has mood-stabilizing effects; at higher doses it acts like an opioid agonist and can cause euphoria and dependence[1][5]. Its mechanism of action was initially thought to involve serotonin reuptake enhancement but more recent research indicates that its main effects are due to modulation of glutamate receptor activity and full agonism at mu opioid receptors[1][5]. It also affects dopamine D2/3 receptors indirectly through downstream pathways. The drug has been associated with significant risks including addiction potential similar to opioids when misused or taken at high doses[2][7].

Brand names
StablonCoaxilTatinolTialeraTianesalTianeurax 12.5mgTianeurax12.5mgTianeurax-12.5mgZinosal
Other names
ZaZa (not official brand)Tianna Red (not official brand)Neptune's Fix (not official brand)tianeptinum natricum (Ph. Eur.)tianeptine sodium (BP/Ph. Eur.)tianeptina generis
02

Targets

DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)iGluR (Ionotropic receptor 76b (Ir76b))

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