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. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
IC50 & Target：
EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)
Room temperature in continental US; may vary elsewhere.
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Varenicline (CP 526555) (subcutaneous injection; 0.01, 0.05, 0.1 and 1 mg/kg; 3 days) iven 10 min prior to nicotine, inhibits nicotine CPP in a dose dependent manner. At the doses of 0.1 and 1 mg/kg totally blocks the effect of nicotine in CPP test without inducing significant changes in preferences on their own.
Varenicline (2.5 mg/kg) results in a place aversion that was dependent on α5 nAChRs but not β2 nAChRs.
Varenicline (0.1 and 0.5 mg/kg) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner.
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.
Bagdas D, et al. New insights on the effects of varenicline on nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology. 2018 Aug;138:72-79.
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