2008•Zhongguo xin yao zazhiRequires access
A partial agonist selective for α_4β_2 nicotinic acetylcholine receptor subtypes,varenicline
Bai Qiu-jiang
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Abstract
Varenicline is a partial agonist selective forα_4β_2 nicotinic aeetylcholine receptor subtypes. Varenicline binds with high affinity and selectivity atα_4β_2 nicotinic acetylcholine receptors.Varenieline blocks the ability of nicotine to activateα_4β_2 receptors and thus blocks the nervous transmission underlying reinforcement and reward experienced upon smoking.Varenicline is used for smoking cessation.This paper introduces mechanism of action,pharmacokinetics,clinical study,drug-drug interactions and adverse effects of varenicline.