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Desvenlafaxine succinate hydrate

CAS: 386750-22-7 F: C20H33NO7 W: 399.48

Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B01
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Bioactivity 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].
Target IC50: 47.3 nM (hSERT), 531.3 nM (hNET).
Invitro 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]. Animal Model:
Name Desvenlafaxine succinate hydrate
CAS 386750-22-7
Formula C20H33NO7
Molar Mass 399.48
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Reference [1]. Darlene C Deecher, et al. Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65. [2]. Michael A Sopko Jr, et al. Desvenlafaxine: another "me too" drug? Ann Pharmacother. 2008 Oct;42(10):1439-46.