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Tianeptine, a tricyclic compound, is a selective facilitator of 5-HT (serotonin; sc-201146) uptake in vitro and in vivo. Additionally, Tianeptine is reported to act as a selective inhibitor of dopamine uptake and is similar to amineptine. Tianeptine does not have a noted effect on monoamine uptake.

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Tianeptine is used in the treatment of reactive and neurotic depression, as well as in the treatment of anxious states.

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Tricyclic compound with psychostimulant, anti-ulcer and anti-emetic properties. Antidepressant

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Tianeptine was identified as an efficacious MOR full agonist, binding to the human MOR with a Ki of 383 ± 183 nM. Tianeptine was also found to act as a full agonist at the DOR, although it had much lower potency and was inactive at the KOR. The MOR was required for the acute and chronic antidepressant-like effects of tianeptine in mice. Although tianeptine also produced behavioural effects, including analgesia and reward, its effects were distinct from morphine in that it did not produce tolerance or withdrawal.

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Taking high doses of tianeptine can cause drowsiness, confusion, difficulty breathing, coma, and death. Long-term use can cause dependence and withdrawal.

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