Desvenlafaxine

Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC₅₀ values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter^[1][2]. IC50 & Target:IC50: 47.3 nM (hSERT), 531.3 nM (hNET)^[1]. In Vitro: Desvenlafaxine has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Desvenlafaxine also induces CYP3A4, which could impact the metabolism of drugs metabolized via this enzyme^[2]. In Vivo: Desvenlafaxine (30 mg/kg, orally) significantly increases extracellular NE levels but had no effect on DA levels using microdialysis^[1].