Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) ( HY-13715 ) and 5-hydroxytryptamine (5-HT) with IC 50 s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. .
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