Varenicline tartrate
Chemical Name: 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
Purity: ≥99%
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
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
Background References
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Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation.
Coe et al.
J.Med.Chem., 2005;48:3474 -
Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid.
Rollema et al.
Neuropharmacology, 2007;52:985 -
Preclinical pharmacology of the α4β2 nAChR partial agonist vareni. related to effects on reward, mood and cognition.
Rollema et al.
Biochem.Pharmacol., 2009;78:813
Product Datasheets
Citations for Varenicline tartrate
The citations listed below are publications that use Tocris products. Selected citations for Varenicline tartrate include:
10 Citations: Showing 1 - 10
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Identification of nicotine-seeking and avoiding larval zebrafish using a new three-choice behavioral assay.
Authors: Andrew Et al.
Front Mol Neurosci 2023;16:1112927
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Gestational ethanol exposure impairs motor skills in female mice through dysregulated striatal dopamine and acetylcholine function.
Authors: David M Et al.
Neuropsychopharmacology 2023;
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Validation of a nicotine vapor self-administration model in rats with relevance to electronic cigarette use.
Authors: Xin Et al.
Neuropsychopharmacology 2020;45:1909-1919
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Direct Effects of Nicotine Exposure on Murine Calvaria and Calvarial Cells.
Authors: Durham Et al.
Sci Rep 2019;9:3805
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Ultrapotent chemogenetics for research and potential clinical applications
Authors: Magnus Et al.
Science 2019;364
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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
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VRC Reduces Context-Induced Relapse to Alcohol-Seeking through Actions in the Nucleus Accumbens.
Authors: Lacroix Et al.
Neuropsychopharmacology 2017;42:1037
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Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP.
Authors: Price Et al.
PLoS One 2015;6:1151
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AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology.
Authors: Cippitelli Et al.
Br J Pharmacol 2015;172:1834
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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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