Varenicline (dihydrochloride)

Varenicline (CP 526555-18) 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

[866823-63-4]

Product Name Alternative

CP 526555 (dihydrochloride)

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

NAChR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/varenicline-dihydrochloride.html

Purity

99.21

Solubility

DMSO : 62.5 mg/mL (ultrasonic) |H2O : ≥ 100 mg/mL

Smiles

[H]Cl.[H]Cl.C1(C2)CNCC2C3=CC4=NC=CN=C4C=C13

Molecular Formula

C13H15Cl2N3

Molecular Weight

284.18

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

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.