LKT Labs

Biochemicals for Life Science Research

Varenicline Tartrate

Product ID V0369
Cas No. 375815-87-5
Purity ≥99%
Product Unit SizeCostQuantityStock
5 mg $76.50 In stock
10 mg $136.90 In stock
25 mg $273.60 In stock
100 mg $912.70 In stock
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Description

Varenicline (VCL) is a modulator of nicotinic acetylcholine receptors (nAChRs) that acts as a partial agonist at α4β2 and α6β2 nAChRs and a full agonist at homomeric α7 nAChRs; VCL may also display agonist activity at β4 nAChR subunits. This compound displays neuromodulatory, cognition enhancing, analgesic, and reward and reinforcement modulating activities. VCL is clinically used as a smoking cessation therapy and is currently under examination as a treatment to decrease alcohol consumption as well. Like other nicotinic agonists, VCL exhibits some cognitive benefit, enhancing working memory in primate models. This compound also induces an analgesic effect in animal models of chronic pain undergoing the formalin test.

Product Info

Cas No.

375815-87-5
Purity

≥99%
Formula

C13H13N3 C4H6O6
Formula Wt.

361.35
Chemical Name

6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino(2,3-h)benzazepine
IUPAC Name

(2R,3R)-2,3-dihydroxybutanedioic acid;5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene
Synonym

Varenicline(Tartrate); Champix; CP 526555-18; Varenicline TaTRate
Appearance

White to off white crystalline powder

Shipping and Storage

Store Temp

Ambient
Ship Temp

Ambient

Downloads

MSDS

V0369 MSDS PDF
Info Sheet

V0369 Info Sheet PDF

References

Hendrickson LM, Guildford MJ, Tapper AR. Neuronal nicotinic acetylcholine receptors: common molecular substrates of nicotine and alcohol dependence. Front Psychiatry. 2013 Apr 30;4:29. PMID: 23641218.

Sotomayor-Zárate R, Gysling K, Busto UE, et al. Varenicline and cytisine: two nicotinic acetylcholine receptor ligands reduce ethanol intake in University of Chile bibulous rats. Psychopharmacology (Berl). 2013 May;227(2):287-98. PMID: 23344555.

Gould RW, Garg PK, Garg S, et al. Effects of nicotinic acetylcholine receptor agonists on cognition in rhesus monkeys with a chronic cocaine self-administration history. Neuropharmacology. 2013 Jan;64:479-88. PMID: 22921923.

AlSharari SD, Carroll FI, McIntosh JM, et al. The antinociceptive effects of nicotinic partial agonists varenicline and sazetidine-A in murine acute and tonic pain models. J Pharmacol Exp Ther. 2012 Sep;342(3):742-9. PMID: 22678099.

Bordia T, Hrachova M, Chin M, et al. Varenicline is a potent partial agonist at α6β2* nicotinic acetylcholine receptors in rat and monkey striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34. PMID: 22550286.

Ortiz NC, O'Neill HC, Marks MJ, et al. Varenicline blocks β2*-nAChR-mediated response and activates β4*-nAChR-mediated responses in mice in vivo. Nicotine Tob Res. 2012 Jun;14(6):711-9. PMID: 22241831.

Xi ZX. Preclinical Pharmacology, Efficacy and Safety of Varenicline in Smoking Cessation and Clinical Utility in High Risk Patients. Drug Healthc Patient Saf. 2010 Apr 1;2010(2):39-48. PMID: 21278851.

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