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Submit ReviewVarenicline tartrate
Description: Selective α4β2 nAChR partial agonist; orally active
Chemical Name: 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
Purity: ≥99% (HPLC)
Biological Activity for Varenicline tartrate
Varenicline tartrate is an 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. Also potently activates PSAM4-5-HT3 and PSAM4-GlyR chimeric ion channels (EC50 values are 4 and 1.6 nM, respectively)
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for Varenicline tartrate
Varenicline tartrate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Varenicline tartrate
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Varenicline tartrate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 36.14 | 100 | |
| DMSO | 18.07 | 50 |
Preparing Stock Solutions for Varenicline tartrate
The following data is based on the product molecular weight 361.37. Batch specific molecular weights may vary from batch to batch due to the degree 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 for Varenicline tartrate
References for Varenicline tartrate
References are publications that support the biological activity of the product.
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 vareni. related to effects on reward, mood and cognition. Biochem.Pharmacol. 78 813 PMID: 19501054
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Keywords: Varenicline tartrate, Varenicline tartrate supplier, nicotinic, receptors, subtype, selective, alpha4beta2, a4b2, α4β2, orally, active, nAChRs, acetylcholine, cholinergics, neuronal, nicotine, Pfizer, chemogenetics, Nicotinic, (a4b2), Receptors, PSEMs, 3754, Tocris Bioscience
7 Citations for Varenicline tartrate
Citations are publications that use Tocris products. Selected citations for Varenicline tartrate include:
Kutlu et al (2018) Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice. Psychopharmacology (Berl) 235 1211 PMID: 29383396
Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications Science 364 PMID: 30872534
Durham et al (2019) Direct Effects of Nicotine Exposure on Murine Calvaria and Calvarial Cells. Sci Rep 9 3805 PMID: 30846819
Lacroix et al (2017) VRC Reduces Context-Induced Relapse to Alcohol-Seeking through Actions in the Nucleus Accumbens. Neuropsychopharmacology 42 1037 PMID: 27834390
Cippitelli et al (2015) AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol 172 1834 PMID: 25440006
Kuryatov et al (2013) Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs. Sci Rep 8 e62246 PMID: 23638015
Price et al (2015) Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP. PLoS One 6 1151 PMID: 25648658
Do you know of a great paper that uses Varenicline tartrate from Tocris? Please let us know.
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