Varenicline-13C15N

Varenicline-13C15N (CP 526555-13C15N) is 13C and 15N labeled 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

[2140265-12-7]

Product Name Alternative

CP 526555-13C15N

UNSPSC

12352005

Target

Isotope-Labeled Compounds; nAChR

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling; Others

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cancer

Smiles

C12=CC3=C(C4CNCC3C4)C=C1[15N]=[13C][13C]=[15N]2

Molecular Formula

C11 13C2H11N 15N2

Molecular Weight

213.22

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]Magnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019;364 (6436) :eaav5282.|[4]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.|[5]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.|[6]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.|[7]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.