This product is freeze dried. All water molecules have been removed.
Every lot is tried & tested in a relevant biological assay.
- 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.
- PNU 282987 (#P-110)
- Ivermectin (#I-110)
- Anti-Nicotinic Acetylcholine Receptor α7 (CHRNA7) (extracellular) Antibody (#ANC-007)
- Anti-Nicotinic Acetylcholine Receptor β2 (CHRNB2) (extracellular) Antibody (#ANC-012)
- Anti-Nicotinic Acetylcholine Receptor β2 (CHRNB2) (extracellular)-ATTO-594 Antibody (#ANC-012-AR)