Varenicline tartrate

Pricing Availability   Qty
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% (HPLC)
Citations (10)
Literature (2)

Biological Activity for Varenicline tartrate

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)

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for Varenicline tartrate

Varenicline tartrate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Varenicline tartrate

M. Wt 361.37
Formula C13H13N3.C4H6O6
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 375815-87-5
PubChem ID 5310966
Smiles OC(C(O)C(O)=O)C(O)=O.C1(C=C([C@H]4CNC[C@@H]3C4)C3=C2)=C2N=CC=N1

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 Data for Varenicline tartrate

Solvent Max Conc. mg/mL Max Conc. mM
water 36.14 100
DMSO 18.07 50

Preparing Stock Solutions for Varenicline tartrate

The following data is based on the product molecular weight 361.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.77 mL 13.84 mL 27.67 mL
5 mM 0.55 mL 2.77 mL 5.53 mL
10 mM 0.28 mL 1.38 mL 2.77 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

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Product Datasheets for Varenicline tartrate

Certificate of Analysis / Product Datasheet
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References for Varenicline tartrate

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

Coe et al (2005) Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 48 3474 PMID: 15887955

Rollema et al (2007) Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 52 985 PMID: 17157884

Rollema et al (2009) Preclinical pharmacology of the α4β2 nAChR partial agonist vareni. related to effects on reward, mood and cognition. Biochem.Pharmacol. 78 813 PMID: 19501054

If you know of a relevant reference for Varenicline tartrate, please let us know.

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Keywords: Varenicline tartrate, Varenicline tartrate supplier, nicotinic, receptors, subtype, selective, alpha4beta2, a4b2, α4β2, orally, active, nAChRs, acetylcholine, cholinergics, neuronal, nicotine, Pfizer, chemogenetics, Nicotinic, (a4b2), Receptors, PSEMs, 3754, Tocris Bioscience

10 Citations for Varenicline tartrate

Citations are publications that use Tocris products. Selected citations for Varenicline tartrate include:

Kutlu et al (2018) Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice. Psychopharmacology (Berl) 235 1211 PMID: 29383396

Andrew et al (2023) Identification of nicotine-seeking and avoiding larval zebrafish using a new three-choice behavioral assay. Front Mol Neurosci 16 1112927 PMID: 37063370

David M et al (2023) Gestational ethanol exposure impairs motor skills in female mice through dysregulated striatal dopamine and acetylcholine function. Neuropsychopharmacology PMID: 37188849

Price et al (2015) Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP. PLoS One 6 1151 PMID: 25648658

Do you know of a great paper that uses Varenicline tartrate from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Nicotinic ACh Receptors Scientific Review

Nicotinic ACh Receptors Scientific Review

Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.

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