PharmGKB summary: venlafaxine pathway

摘要

Venlafaxine (VEN) is a serotonin-norepinephrine re-uptake inhibitor marketed for the treatment of depression disorders. The molecular targets of VEN are the solute carrier family 6 (neurotransmitter transporter, serotonin), member 4 (SLG6A4), and solute carrier family 6 (neurotransmitter transporter, noradrenalin), member 2 (SLG6A2), resulting in an inhibition of serotonin and noradrenaline reuptake from the synaptic cleft. VEN also slightly inhibits dopamine reuptake. Therefore, those substances are available prolonged in the synaptic cleft for serotonergic and noradrenergic neurotransmission. VEN consists of a racemic mixture of R(+) and S(-) enantiomer. The (R) enantiomer has been shown to show greater serotonin reuptake inhibition property, whereas the (S) enantiomer inhibits the reuptake of both monoamines [1,2].