Biological Activity
Orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 361.37 |
| Formula | C13H13N3.C4H6O6 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 375815-87-5 |
| PubChem ID | 5310966 |
| InChI Key | JQSHBVHOMNKWFT-DTORHVGOSA-N |
| Smiles | OC(C(O)C(O)=O)C(O)=O.C1(C=C([C@H]4CNC[C@@H]3C4)C3=C2)=C2N=CC=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.07 | 50 | |
| water | 36.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 361.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.77 mL | 13.84 mL | 27.67 mL |
| 5 mM | 0.55 mL | 2.77 mL | 5.53 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.77 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Coe et al (2005) Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 48 3474 PMID: 15887955
Rollema et al (2007) Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 52 985 PMID: 17157884
Rollema et al (2009) Preclinical pharmacology of the α4β2 nAChR partial agonist varenicline related to effects on reward, mood and cognition. Biochem.Pharmacol. 78 813 PMID: 19501054
Keywords: Varenicline tartrate, supplier, nicotinic, receptors, subtype, selective, alpha4beta2, a4b2, α4β2, orally, active, nAChRs, acetylcholine, cholinergics, neuronal, nicotine, Pfizer, Nicotinic, (a4b2), Receptors, Nicotinic, (a4b2), Receptors, Tocris Bioscience
