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    Vilazodone HCl (EMD 68843; SB659746A)
    Vilazodone HCl (EMD 68843; SB659746A)

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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 #: V0972
    CAS #: 163521-08-2Purity ≥98%

    Description: Vilazodone HCl (SB659746A; SB659746-A; EMD-68843; EMD68843; Viibryd), the hydrochloride salt of Vilazodone, is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors with anti-depressive effects. As of 2011, Vilazodone was approved by the FDA to treat major depressive disorders. Vilazodone demonstrates an IC50 of 0.2 nM at the human 5-HT1A receptor and 0.5 nM for the SERT. Vilazodone displays high affinity (pKi ≥ 9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A receptors. 

    References: CNS Neurosci Ther. 2009 Summer;15(2):107-17; Eur J Pharmacol. 2005 Mar 7;510(1-2):49-57.

    Related CAS: 163521-12-8 (free base); 1794789-93-7 (Vilazodone D8); 163521-19-5 (Vilazodone carboxylic acid)

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    Molecular Weight (MW)477.99
    FormulaC26H27N5O2.HCl 
    CAS No.163521-08-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 96 mg/mL (200.8 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    SMILES CodeO=C(C1=CC2=CC(N3CCN(CCCCC4=CNC5=C4C=C(C#N)C=C5)CC3)=CC=C2O1)N.[H]Cl
    SynonymsEMD68843; SB659746A; SB659746-A; EMD-68843; EMD68843; SB659746 A; Vilazodone hydrochloride; Viibryd


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    In Vitro

    In vitro activity: Vilazodone demonstrates an IC50 of 0.2 nM at the human 5-HT1A receptor and 0.5 nM for the SERT. Vilazodone displays high affinity (pKi ≥ 9.3) for human recombinant and rat, guinea pig, mouse, and marmoset native tissue 5-HT1A receptors.


    Cell Assay: Administration of 5-HT1A receptor agonists produce a characteristic behavioral syndrome that includes changes in posture, hind limb reduction, head weaving, tremors, forepaw treading, and straub tail. In the rat ultrasonic vocalizations test, stress-induced vocalizations are inhibited by Vilazodone (55 mg/kg po) at 120 and 210 min post dose. Vilazodone (20-40 mg/kg ip), administered acutely or prophylactically (1 week prior to behavioral testing), attenuated stress induces potentiated startle but has no effect on stress potentiated anxiety response in the elevated plus maze. Interestingly, a lower dose of 10 mg/kg of Vilazodone has the opposite effect in the startle response, indicating a somewhat unexplained bidirectional effect, and all doses produce a potentiation of the startle-induced stress response possibly suggestive of an anxiogenic-like response[1]. Vilazodone also represents another option for the treatment of MDD.

    In VivoVilazodone selectively enhances serotonergic output in the prefrontal cortex of rats. Vilazodone demonstrates anxiolytic efficacy through Behavioral evaluations in the ultrasonic vocalization model of anxiety in rats. Vilazodone also shows efficacy but at a single dose only in the forced swim test (a putative model of depression). Vilazodone (1-10 mg/kg p.o.) dose-dependently displaces in vivo [3H]DASB (N,N-dimethyl-2-(2-amino-4-cyanophenylthio)benzylamine) binding from rat cortex and hippocampus, indicating that vilazodone occupies 5-HT transporters in vivo. Vilazodone (10 mg/kg p.o.) is demonstrated to cause a 2-fold increase in extracellular 5-HT but no change in noradrenaline or dopamine levels in frontal cortex of freely moving rats. Vilazodone affects stress potentiation of startle at doses above 5 mg/kg in rats. Vilazodone increases stress elevation of startle at 10 mg/kg in rats. Vilazodone (20 and 40 mg/kg) blocked stress potentiation of startle in rats. Vilazodone increases stress elevation of startle at all doses in rats. Vilazodone has no effect on 5-HT efflux at 100 nM but significantly decreases 5-HT efflux at 1 mM in the guinea-pig dorsal raphe nucleus. Vilazodone significantly increases the re-uptake half life for 5-HT in the guinea-pig dorsal raphe nucleus.
    Animal model Rats
    Formulation & Dosage 1-10 mg/kg; p.o.
    ReferencesCNS Neurosci Ther. 2009 Summer;15(2):107-17; Eur J Pharmacol. 2005 Mar 7;510(1-2):49-57.


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

     

    Vilazodone HCl

    Eur J Pharmacol. 2005 Mar 7;510(1-2):49-57.
     

    Vilazodone HCl

    Eur J Pharmacol. 2005 Mar 7;510(1-2):49-57.


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