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Article

Varenicline blocks β2-nAChR-mediated response and activates β4-nAChR-mediated responses in mice in vivo.

Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco - 1 Jun 2012

Ortiz Nick C, O'Neill Heidi C, Marks Michael J, Grady Sharon R

Abstract excerpt

INTRODUCTION: 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. METHODS:...

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Identifiers

PMID: 22241831
DOI: 10.1093/ntr/ntr284
PMCID: PMC3356295

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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