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.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 361.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|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|
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 varenicline 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.
View Related Products by Product Action
Keywords: Varenicline tartrate, Varenicline tartrate supplier, nicotinic, receptors, subtype, selective, alpha4beta2, a4b2, α4β2, orally, active, nAChRs, acetylcholine, cholinergics, neuronal, nicotine, Pfizer, Nicotinic, (a4b2), Receptors, 3754, Tocris Bioscience
3 Citations for Varenicline tartrate
Citations are publications that use Tocris products. Selected citations for Varenicline tartrate include:
Cippitelli et al (2015) AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol 172 1834 PMID: 25440006
Kuryatov et al (2013) Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs. Sci Rep 8 e62246 PMID: 23638015
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.
Reviews for Varenicline tartrate
There are currently no reviews for this product. Be the first to review Varenicline tartrate and earn rewards!
Have you used Varenicline tartrate?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.