Varenicline

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Scientific Name: Varenicline
Brand Name: Champix, Chantix, Tyrvaya
Company Owner: Not Available
Mechanism Of Action Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectivity for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20, 000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold) . The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms.
Description of the Drug: Varenicline is a partial agonist at nicotinic acetylcholine receptors used as an aid in smoking cessation.
Protein Data Bank:
Source: DrugBank Online – DrugBank.com. Retrieved 2023-01-23 from https://go.drugbank.com/drugs/DB01273