Varenicline (Standard)

Varenicline (Standard) is the analytical standard of Varenicline. This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation[1][2][3][4][5].

Product Specifications

CAS Number

[249296-44-4]

Product Name Alternative

CP 526555 (Standard)

UNSPSC

12352005

Target

NAChR; Reference Standards

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling; Others

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cancer

Smiles

C12=C(C=C3N=CC=NC3=C2)C4CC1CNC4

Molecular Formula

C13H13N3

Molecular Weight

211.27

References & Citations

[1]Koegelenberg CF, et al. Efficacy of varenicline combined with nicotine replacement therapy vs varenicline alone for smoking cessation: a randomized clinical trial. JAMA. 2014 Jul;312 (2) :155-61.|[2]Magnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019;364 (6436) :eaav5282.|[3]Koga M, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017;390:1-9.|[4]Ren J, et al. Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Anesthesiology. 2020 May;132 (5) :1197-1211.|[5]Mello NK, et al. Effects of chronic varenicline treatment on nicotine, cocaine, and concurrent nicotine+cocaine self-administration. Neuropsychopharmacology. 2014 Apr;39 (5) :1222-31.|[6]Rollema H, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect. Eur J Pharmacol. 2009 Mar 1;605 (1-3) :114-6.