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).1 Formulations containing varenicline have been used as aids in smoking cessation.
1.Mihalak, K.B., Carroll, F.I., and Luetje, C.W.Varenicline is a partial agonist at α4β2 and a full agonist at α7 neuronal nicotinic receptorsMol. Pharm.70(3)801-805(2006)