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    Varenicline Tartrate (CP 526555-18)
    Varenicline Tartrate (CP 526555-18)

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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 #: V1203
    CAS #: 375815-87-5Purity ≥98%

    Description: Varenicline Tartrate (CP-526555 18; CP 526555 18; Chantix; Champix), the tartrate salt of varenicline, is a potent partial agonist of nicotinic AChR (acetylcholine receptor) used for smoke-cessation and nicotine addiction. 

    References: Neuropharmacology. 2007 Mar;52(3):985-94; Psychopharmacology (Berl). 2010 Feb;208(3):365-76.

    Related CAS #: 375815-87-5 (tartrate)   249296-44-4 (free)   230615-23-3 (HCl) 

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    • 香港大学
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    Molecular Weight (MW)361.35 
    FormulaC13H13N3·C4H6O6 
    CAS No.375815-87-5 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: 72 mg/mL (199.3 mM) 
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: (6R,10S)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline (2R,3R)-2,3-dihydroxysuccinate

    InChi Key: TWYFGYXQSYOKLK-CYUSMAIQSA-N

    InChi Code: InChI=1S/C13H13N3.C4H6O6/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;5-1(3(7)8)2(6)4(9)10/h1-2,4-5,8-9,14H,3,6-7H2;1-2,5-6H,(H,7,8)(H,9,10)/t8-,9+;1-,2-/m.1/s1

    SMILES Code: C1[[email protected]@H]2CNC[[email protected]]1C3=CC4=NC=CN=C4C=C23.[[email protected]@H]([[email protected]](C(=O)O)O)(C(=O)O)O           

    SynonymsCP 526555-18; CP52655518; Varenicline tartrate; CP-526555 18; CP 526555 18; Chantix; Champix


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    In Vitro

    In vitro activity: Varenicline is a partial agonist with 45% of nicotine's maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 mM and an efficacy of 75%.

    In VivoVarenicline has significantly lower (40-60%) efficacy than nicotine in stimulating [(3)H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than Nicotine. Varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of Varenicline alone, consistent with partial agonism. Varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. Varenicline, a partial agonist at thealpha4beta2 nAChRs, reduces nicotine intake and was recently approved as a smoking cessation aid. Varenicline selectively reduces ethanol but not sucrose seeking using an operant self-administration drinking paradigm and also decreases voluntary ethanol but not water consumption in animals chronically exposed to ethanol for 2 months before Varenicline treatment. 
    Animal modelRats
    Formulation & Dosage
    References

    Neuropharmacology. 2007 Mar;52(3):985-94; Psychopharmacology (Berl). 2010 Feb;208(3):365-76. 


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

    Varenicline Tartrate

    The effects of varenicline on food self-administration under a fixed ratio schedule of reinforcement. Psychopharmacology (Berl). 2010 Feb;208(3):365-76.


    Varenicline Tartrate

    The effects of varenicline on nicotine self-administration under a fixed ratio schedule of reinforcement.
     

    Varenicline Tartrate

    The effects of varenicline on reinstatement of nicotine-seeking. Psychopharmacology (Berl).2010 Feb;208(3):365-76.
     

    Varenicline Tartrate

    Dose–response functions for nicotine and varenicline prime-induced reinstatement of nicotine seeking. Psychopharmacology (Berl).2010 Feb;208(3):365-76.


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