Varenicline tartrate

Name: Varenicline tartrate
Brand: Tocris Bioscience
SKU: 3754

Tocris Bioscience, part of Bio-Techne | Catalog # 3754

Citations (25)

COA / SDS

Selective α4β2 nAChR partial agonist; orally active

Key Product Details

Chemical Name:	7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
Purity:	≥99%
Molecular Weight:	361.37 kDa

View Full Technical Details for Varenicline tartrate

Technical Data
Citations

Biological Activity for Varenicline tartrate

Varenicline tartrate is an orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (K_i 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 for Varenicline tartrate

M. Wt	361.37 kDa
Formula	C₁₃H₁₃N₃.C₄H₆O₆
Storage	Desiccate at RT
Purity	≥99%
CAS Number	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.

Solubility for Varenicline tartrate

Solubility

Soluble Soluble to 100 mM in water and to 50 mM in DMSO

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References for Varenicline tartrate

References are publications that support the biological activity of the product.

Coe et al. Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem., 2005;48:3474 PMID: 15887955
Rollema et al. Pharmacological profile of the α₄β₂ nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology, 2007;52:985 PMID: 17157884
Rollema et al. Preclinical pharmacology of the α4β2 nAChR partial agonist vareni. related to effects on reward, mood and cognition. Biochem.Pharmacol., 2009;78:813 PMID: 19501054