Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor ( IC 50 = 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors ( K i =4.2 μM) and agonizes 5-HT2C receptors ( EC 50 = 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD).
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