Overview
- Mihalak, K.B. et al. (2006) Mol. Pharmacol. 70, 801.
- De Biasi, M. and Salas, R. (2008) Exp. Biol. Med. 233, 917.
Alomone Labs Varenicline tartrate activates α7 nicotinic acetylcholine receptor channels heterologously expressed in Xenopus oocytes.Current traces of α7 nicotinic acetylcholine receptor channels activity at -60 mV holding potential. 100 μM Varenicline tartrate (#V-105) alone activates a transient relatively small current (right), while perfusing PNU-120596 prior to Varenicline tartrate activates a much larger current (left), even at a 10 fold lower concentration (middle). Periods of compound perfusion are indicated by the horizontal bars: PNU; PNU-120596, VAR; Varenicline tartrate.
- Mihalak, K.B. et al. (2006) Mol. Pharmacol. 70, 801.
- Rollema, H. et al. (2007) Neuropharmacology 52, 985.
- Papke, R.L. et al. (2010) J. Pharmacol. Exp.Ther. 333, 501.
- De Biasi, M. and Salas, R. (2008) Exp. Biol. Med. 233, 917.
- Nides, M. et al. (2006) Arch. Intern. Med. 166, 1561.
- Foulds, J. (2006) Int. J. Clin. Pract. 60, 571.
Varenicline tartrate is a partial agonist of α4/β2 nicotinic Acetylcholine receptors (nAChR) and a full agonist of a7 nAChR1, it is also an effective activator of α3/β4 receptors with apparent EC50 in the mM range2,3. Based on these characteristics, especially the partial agonistic activity towards the α4/β2 nAChR, it may be suitable for treating nicotine addiction4-6.
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 α4/β2 nAChRs and inhibited the nicotine induced currents2. In addition, varenicline reduced nicotine self-administration in rats2.
Varenicline tartrate (#V-105) is a highly pure, synthetic, and biologically active compound.
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