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    Desvenlafaxine (WY 45233; O-Desmethylvenlafaxine)
    Desvenlafaxine (WY 45233; O-Desmethylvenlafaxine)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1034
    CAS #: 93413-62-8Purity ≥98%

    Description: Desvenlafaxine (WY-45233; WY45233; brand names Pristiq, Desfax), the active metabolite of the antidepressant venlafaxine, is a potent inhibitor/antagonist of the reuptake of serotonin (5-HT) transporter and norepinephrine (NE) transporter with Ki of 40.2 nM and 558.4 nM respectively. 

    References: J Pharmacol Exp Ther. 2006 Aug;318(2):657-65; Ann Pharmacother. 2008 Oct;42(10):1439-46.

    Related CAS#:448904-47-0 (succinate); 386750-22-7 (Succinate hydrate); 300827-87-6 (HCl); 93414-04-1 (fumarate); 1147940-37-1 (benzoate)

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    Molecular Weight (MW)263.38
    FormulaC16H25NO2
    CAS No.93413-62-8  (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 37 mg/mL (140.5 mM)
    Water: <1 mg/mL
    Ethanol: 3 mg/mL (11.4 mM)
    Solubility (In vivo)0.5% methylcellulose+0.2% Tween 80: 30 mg/mL  
    SynonymsWY-45233; WY45233; WY 45233; Pristiq; Desfax


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    In Vitro

    In vitro activity: Desvenlafaxine is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, desvenlafaxine inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with desvenlafaxine, which could impact the metabolism of drugs metabolized via this enzyme.

    In VivoDesvenlafaxine rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. Desvenlafaxine exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5%.
    Animal model Male Sprague-Dawley rats 
    Formulation & DosageDissolved in 0.25% Tween 80 and 0.5% methylcellulose; 30 mg/kg; oral gavage
    ReferencesJ Pharmacol Exp Ther. 2006 Aug;318(2):657-65; Ann Pharmacother. 2008 Oct;42(10):1439-46. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Desvenlafaxine

    DVS competes for the binding of radioligands specific to the serotonin (membrane) (A) and norepinephrine (whole-cell) (B) transporters, whereas weak competition was noted for the radioligand specific to the dopamine (membrane) (C) transporter. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65.

    Desvenlafaxine

    A-C, DVS increases extracellular levels of serotonin (A) and norepinephrine (B) without increasing dopamine (C) in the rat hypothalamus compared with baseline. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65.

     

    Desvenlafaxine
    Orally administered desvenlafaxine (30 mg/kg) to intact male rats is found in plasma and penetrates the brain and hypothalamus over time.
    Desvenlafaxine
    Functional activity of desvenlafaxine demonstrates inhibition of radioligand uptake of serotonin (A) or norepinephrine (B). For each uptake transporter bioassay, a known comparator was used [fluoxetine (5-HT reuptake inhibitor) and desipramine (NE reuptake inhibitor)]. Each data point depicted represents the mean ± S.E.M. of three independent experiments performed in triplicate. J Pharmacol Exp Ther. 2006 Aug;318(2):657-65.


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