varenicline hydrochloride

Varenicline Hydrochloride (CP 526555) is an orally active partial agonist of the α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is recognized as the principal mediator of nicotine dependence, and its pharmacological effect is critical in modulating addictive behaviors associated with nicotine exposure. Varenicline Hydrochloride (CP 526555) blocks the direct agonist effects of nicotine on nicotinic acetylcholine receptors while simultaneously stimulating these receptors in a more moderate and controlled manner, making it a widely used research compound in smoking cessation.

Varenicline-d4hydrochloride is a deuterium-labeled form of Varenicline (dihydrochloride). Varenicline (CP 526555) dihydrochloride acts as a partial agonist for the α4β2 nicotinic acetylcholine receptor (α4β2nAChR), with an EC50 of 2.3 μM. It serves as a full agonist for α3β4nAChR and α7nAChR, with EC50 values of 55 μM and 18 μM, respectively. As a nicotine ligand based on a cytosine structure, Varenicline dihydrochloride is utilized in smoking cessation research.