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The smoking cessation aid, varenicline, has higher affinity for the alpha4beta2-subtype of the nicotinic acetylcholine receptor (α4β2*-nAChR) than for other subtypes of nAChRs by in vitro assays. The mechanism of action of acute varenicline was studied in vivo to determine (a) subtype activation associated with physiological effects and (b) dose relationship as an antagonist of nicotine.

Varenicline Blocks 2*-nAChR-Mediated Response and Activates 4*-nAChR-Mediated Responses in Mice In Vivo

Varenicline Blocks 2-nAChR-Mediated Response and Activates 4-nAChR-Mediated Responses in Mice In Vivo