Name: Varenicline
Price: 300.00 USD

- Overview
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    Background
    
    Varenicline is a partial agonist/antagonist of α4β2 nicotinic acetylcholine receptor [1].Varenicline is a manufactured tartrate salt, it is a partial agonist of α4β2 nAChRs. The affinity(0.15 nM) of varenicline with α4β2 nAChRs is much more higher than with other nAChR subtypes. Through the binding, varenicline prevents nicotine from occupying the receptors and subsequently inhibit nicotine-induced dopaminergic activation. So varenicline is used for smoking cessation. In healthy adult smokers, varenicline does not undergo significant hepatic metabolism and the clearance(>90%) is predominantly renal. It is shown that the amphetamine administration may have decrease the efficacy of varenicline [1].
    
    [1] Garrison GD, Dugan SE. Varenicline: a first-line treatment option for smoking cessation. Clin Ther. 2009 Mar;31(3):463-91.
- Properties
  - Categories
    
    α4β2 nAChRs antagonist
    
    Alternative Name
    
    (6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline
    
    CAS Number
    
    249296-44-4
    
    Molecular Formula
    
    C13H13N3
    
    Molecular Weight
    
    211.26
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    [H]C1(C([H])([H])N([H])C2([H])[H])C([H])([H])[[email protected]]2([H])C3=C([H])C4=NC([H])=C([H])N=C4C([H])=C13
    
    * For Research Use Only