Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.
Varenicline induces dose-dependent and sustains increases in striatal DRD2/3 in rats, particularly in the ventral striatum.[2]
[1] Mihalak KB, et al. Mol Pharmacol. 2006 Sep;70(3):801-5. [2] Crunelle CL, et al. Eur Neuropsychopharmacol. 2011 Feb;21(2):205-10.
















