6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 6,7,8,9-tetrahydro-, monohydrochloride

Uses

Varenicline Hydrochloride is a useful nicotine binding inhibitor.

Biological Activity

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].

References

[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.