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Varenicline tartrate

Catalog #: 3754
7 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
3754/10
3754/50
Varenicline tartrate | CAS No. 375815-87-5 | Nicotinic (a4b2) Receptor Agonists
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Description: Selective α4β2 nAChR partial agonist; orally active

Chemical Name: 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate

Purity: ≥99%

Product Details
Citations (7)
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Biological Activity

Varenicline tartrate is an 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. Also potently activates PSAM4-5-HT3 and PSAM4-GlyR chimeric ion channels (EC50 values are 4 and 1.6 nM, respectively)

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

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Citations for Varenicline tartrate

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

7 Citations: Showing 1 - 7

  1. Direct Effects of Nicotine Exposure on Murine Calvaria and Calvarial Cells.
    Authors: Durham Et al.
    Sci Rep  2019;9:3805
  2. Ultrapotent chemogenetics for research and potential clinical applications
    Authors: Magnus Et al.
    Science  2019;364
  3. Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice.
    Authors: Kutlu Et al.
    Psychopharmacology (Berl)  2018;235:1211
  4. VRC Reduces Context-Induced Relapse to Alcohol-Seeking through Actions in the Nucleus Accumbens.
    Authors: Lacroix Et al.
    Neuropsychopharmacology  2017;42:1037
  5. Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP.
    Authors: Price Et al.
    PLoS One  2015;6:1151
  6. AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology.
    Authors: Cippitelli Et al.
    Br J Pharmacol  2015;172:1834
  7. 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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VersaClone cDNA Plasmids

Human nAChR alpha 4/CHRNA4 (NP_000735) VersaClone cDNA

RDC0281

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