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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)
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for Varenicline tartrate
Technical Data for Varenicline tartrate
|Storage||Desiccate at RT|
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|
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.
|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|
Product Datasheets for Varenicline tartrate
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
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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
7 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
Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications Science 364 PMID: 30872534
Durham et al (2019) Direct Effects of Nicotine Exposure on Murine Calvaria and Calvarial Cells. Sci Rep 9 3805 PMID: 30846819
Cippitelli et al (2015) AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol 172 1834 PMID: 25440006
Lacroix et al (2017) VRC Reduces Context-Induced Relapse to Alcohol-Seeking through Actions in the Nucleus Accumbens. Neuropsychopharmacology 42 1037 PMID: 27834390
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
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
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Literature in this Area
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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.