BUY Varenicline tartrate

Varenicline tartrate. A Partial Agonist of alpha4/beta2 nAChR.

Varenicline tartrate is a partial agonist of alpha4/beta2 nicotinic Acetylcholine receptors (nAChR) and a full agonist of alpha7 nAChR, it is also an effective activator of alpha3/beta4 receptors with apparent EC₅₀ in the μM range.
Based on these characteristics, especially the partial agonistic activity towards the alpha4/beta2 nAChR, it may be suitable for treating nicotine addiction.
In vitro functional patch clamp studies in HEK cells expressing nAChRs show that varenicline is a partial agonist with 45% of nicotine's maximal efficacy at alpha4/beta2 nAChRs and inhibited the nicotine induced currents.
In addition, varenicline reduced nicotine self-administration in rats.

Ion Channel Modulators; Nicotinic Acetylcholine Receptor Activators