Levomilnacipran Hydrochloride

Nobody knows exactly how levomilnacipran works as an antidepressant. It is thought to act by increasing the effect of serotonin and norepinephrine in the central nervous system, because it blocks their reuptake at the serotonin and norepinephrine transporters. Non-clinical studies have shown that levomilnacipran is a potent and selective serotonin and norepinephrine reuptake inhibitor (SNRI).

Levomilnacipran binds with high affinity to the human serotonin (5-HT) and norepinephrine (NE) transporters (Ki = 11 and 91 nM, respectively), and it strongly inhibits the reuptake of 5-HT and NE (IC50 = 16 to 19 and 11 nM, respectively). In the in vitro tests, it showed no significant affinity for any other receptors, ion channels or transporters. This included serotonergic (5HT1-7), α- and β-adrenergic, muscarinic and histaminergic receptors, and Ca2+, Na+, K+ or Cl- channels. Levomilnacipran also did not inhibit monoamine oxidase (MAO).