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    Desvenlafaxine Succinate (WY 45233; O-Desmethylvenlafaxine)
    Desvenlafaxine Succinate (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 #: V1033
    CAS #: 448904-47-0 Purity ≥98%

    Description: Desvenlafaxine Succinate (formerly WY45233; WY 45233; O-desmethylvenlafaxine; trade name Pristiq, Desfax), the succinate salt of Desvenlafaxine which is an approved antidepressant drug, is a novel and potent serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively. Desvenlafaxine is the active metabolite of the antidepressant venlafaxine (sold under the trade names Effexor and Efexor). 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 is being targeted as the first non-hormonal based treatment for menopause.

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

    Related CAS#: 93413-62-8 (free base); 448904-47-0 (succinate); 300827-87-6 (HCl); 93414-04-1 (fumarate); 1147940-37-1 (benzoate); 386750-22-7 (Succinate hydrate)  

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    Molecular Weight (MW)381.46 
    FormulaC16H25NO2.C4H6O4.H2O 
    CAS No.386750-22-7 (Succinate hydrate);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (209.7 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)0.5% methylcellulose+0.2% Tween 80: 30 mg/mL  
    SynonymsWY 45233 Succinate; WY-45233; Pristiq; WY45233; WY 45233; Desfax


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    In Vitro

    In vitro activity: Desvenlafaxine succinate is the succinate salt monohydrate of O-desmethylvenlafaxine, an active metabolite of venlafaxine. Desvenlafaxine Succinate is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, Desvenlafaxine Succinate inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine Succinate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine Succinate inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine Succinate 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 Succinate, which could impact the metabolism of drugs metabolized via this enzyme.

    In VivoDesvenlafaxine Succinate rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine Succinate significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. Desvenlafaxine Succinate 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 modelMale 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 Succinate

    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 Succinate

    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 Succinate
    Orally administered desvenlafaxine (30 mg/kg) to intact male rats is found in plasma and penetrates the brain and hypothalamus over time.


    Desvenlafaxine Succinate
    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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