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Cat. No. Name Size Price Add Cart
KI0899Varenicline tartrate5 mg$154
Varenicline tartrate10 mg$272

Chemical Characteristic

Product NameVarenicline tartrate
SynonymsChantix, Champix
CAS No.375815-87-5
Molecular Weight 361.35
FormulaC17H19N3O6
Chemical Structure

Biological activities

Varenicline tartrate is a subtype-selective partial agonist at α4β2 nicotinic receptors. Varenicline tartrate is used to treat smoking addiction. The Ki values of varenicline tartrate are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors, respectively. Varenicline tartrate (10 µM) is shown to act as agonists with lower efficacy than 10 µM nicotine with 68% response of nicotine.[1] In vitro functional patch clamp studies in HEK cells expressing nAChRs, varenicline tartrate is a partial agonist with 45% of nicotine's maximal efficacy at α4β2 nAChRs. In neurochemical models varenicline tartrate has significantly lower (40-60%) efficacy than nicotine in stimulating [3H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo. In addition, when combined with nicotine, varenicline tartrate effectively attenuates the nicotine-induced dopamine release to the level of the effect of varenicline alone, consistent with partial agonism.[2] In vivo, varenicline tartrate treatment (5.6 mg/kg s.c) has 32% of the maximal nicotine response on dopamine turnover.[1]Varenicline tartrate has anxiolytic effects in the marble-burying test and in the novelty-induced hypophagia (NIH) test.[3]

Protocols

In vivo: Varenicline tartrate is dissolved in sterile 0.9% saline solution.[3]

References

[1] Coe JW, et al. Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 2005, 48(10): 3474-3477. 閵嗏偓閵嗏偓
[2] Rollema H, et al. Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology. 2007, 52(3): 985-994.
[3] Turner JR, et al. Nicotinic partial agonists varenicline and sazetidine-A have differential effects on affective behavior. J Pharmacol Exp Ther. 2010, 334(2): 665-672. 閵嗏偓閵嗏偓

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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