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Overview
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Background
Varenicline Hydrochloride is a partial agonist of α4β2 nicotinic receptor for smoking cessation [1].Varenicline Hydrochloride has been reported to potently inhibit nAChR binding with the Ki values of 0.12±0.02 nM and 0.14±0.01 nM for α6β2* nAChR and α4β2* nAChR, respectively in rat striatum, 0.13±0.01 nM and 0.19±0.11 nM forα6β2* nAChR and α4β2* nAChR, respectively in monkey striatum. In addition, varenicline Hydrochloride has shown to be more potent in stimulating both α6β2* and α4β2* nAChRs compared with nicotine with the EC50 values of 0.007 and 0.086μM, respectively in rat striatum [1].
[1] Bordia T1, Hrachova M, Chin M, McIntosh JM, Quik M. Varenicline is a potent partial agonist at α6β2* nicotinic acetylcholine receptors in rat and monkey striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34. doi: 10.1124/jpet.112.194852. Epub 2012 May 1.
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- Properties
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Overview