Varenicline

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

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

NAChR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Varenicline.html

Purity

99.92

Solubility

DMSO : 20 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C13H13N3

Molecular Weight

211.27

Precautions

H315, H319, H320

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.