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Vortioxetine


Mechanism of action:

Vortioxetine is a serotonin modulator. Vortioxetine inhibits the serotonin transporter in neurons, preventing serotonin reuptake and increasing the concentration of serotonin (5-HT) in the synaptic cleft, thereby enhancing serotonergic activity. Vortioxetine also acts directly on multiple 5-HT receptors: it is an agonist at the 5-HT1A receptor, a partial agonist at the 5-HT1B receptor, and an antagonist at the 5-HT3 and 5-HT7 receptors, collectively modulating the depressive state.

Reference(s):

1. Bang-Andersen B et al. (2011). Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 


2. Stenkrona P et al. (2013). 5-HTT and 5-HT(1A) receptor occupancy of the novel substance vortioxetine (Lu AA21004). A PET study in control subjects. Eur Neuropsychopharmacol. 


3. Mork A et al. (2013). Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacol Biochem Behav.

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