Catalog Number: 3754
Chemical Name: 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
Biological Activity
Orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo.
Technical Data
  • M.Wt:
    361.37
  • Formula:
    C13H13N3.C4H6O6
  • Solubility:
    Soluble to 100 mM in water and to 50 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    375815-87-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation.
    Coe et al.
    J.Med.Chem., 2005;48:3474
  2. Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid.
    Rollema et al.
    Neuropharmacology, 2007;52:985
  3. Preclinical pharmacology of the α4β2 nAChR partial agonist varenicline related to effects on reward, mood and cognition.
    Rollema et al.
    Biochem.Pharmacol., 2009;78:813
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Varenicline tartrate include:

2 Citations: Showing 1 - 2
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  1. Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP.
    Authors: Price Et al.
    PLoS One 2015;6:1151
  2. Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs.
    Authors: Kuryatov Et al.
    Sci Rep 2013;8:e62246

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