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Levomilnacipran is an active enantiomer of the serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor milnacipran (Item No. 23837).1 It binds to the 5-HT and NE transporters (Kis = 11.2 and 92.2 nM, respectively, for human recombinant transporters) and inhibits reuptake in vitro (IC50s = 19 and 10.5 nM, respectively). It is selective for 5-HT and NE transporters over DAT (Ki = >10,000 nM for human recombinant DAT) and 23 receptors (Kis = ≥10,000 nM). Levomilnacipran increases extracellular levels of 5-HT and NE in rat cortex with minimal effective doses (MEDs) of 20 and 10 mg/kg, respectively. It decreases immobility in the forced swim and tail suspension tests (MEDs = 20 and 2.5 mg/kg, respectively) without increasing locomotor activity. Formulations containing levomilnacipran have been used in the treatment of major depressive disorder.
WARNING This product is not for human or veterinary use.
1. Levomilnacipran (F2695), a norepinephrine-