Desvenlafaxine (succinate hydrate)

Desvenlafaxine succinate hydrate, 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 succinate hydrate 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 succinate hydrate has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Desvenlafaxine succinate hydratealso induces CYP3A4, which could impact the metabolism of drugs metabolized via this enzyme^[2]. In Vivo: Desvenlafaxine succinate hydrate (30 mg/kg, orally) significantly increases extracellular NE levels but had no effect on DA levels using microdialysis^[1].