Varenicline-d4

Varenicline-d₄ is intended for use as an internal standard for the quantification of varenicline by GC- or LC-MS. Varenicline is a full agonist of α7 subunit-containing neuronal nicotinic acetylcholine receptors (nAChRs; EC₅₀ = 18 μM) and a partial agonist of α4β2 subunit-containing nAChRs (EC₅₀ = 2.3 μM). Formulations containing varenicline have been used as aids in smoking cessation.

Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].

[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. DOI:10.1177/1060028018797110
[2] Mihalak KB, et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.Mol Pharmacol.2006 Sep;70(3):801-5. Epub 2006 Jun 9. DOI:10.1124/mol.106.025130
[3] Bagdas D, et al. New insights on the effects ofvareniclineon nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology.2018 Aug;138:72-79. DOI:10.1016/j.neuropharm.2018.05.025