Tianeptine is an agonist at μORs and δORs as well as a potentiator at D2 and D3 DA receptors. Tianeptine exhibits neuromodulatory, antidepressant, anxiolytic, analgesic, anticonvulsant, and anti-inflammatory activities, although its mechanism of action is not well understood. In vitro, tianeptine inhibits LPS-induced inflammation and activation of microglia; is also decreases pro-inflammatory cytokine release, ROS release, and NF-κB activation. Clinically, this compound improves anxiety symptoms, neurocognitive function, and memory. Tianeptine also attenuates mechanical allodynia, an effect that may be mediated by 5-HT7 receptors.