
Supplier:
Alomone Labs Ltd.Cat no: V-105
Varenicline tartrate
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
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