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Varenicline tartrate
Cat. No. NA-030
Structure:
7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline tartrate:7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine tartrate
Other Names:
Chantix; CP-526,555-18
Activity:
α4ß2 partial agonist
Varenicline tartrate is an orally active, subtype-selective partial agonist at α4β2 nicotinic receptors with Ki values of 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively, and a full agonist at α7 neuronal nicotinic receptors. In humans, following oral administration, varenicline is almost completely absorbed and has high bioavailability (90%). Varenicline stimulates basal mesolimbic dopamine release to approximately 50% of the maximal effect of nicotine, inhibits nicotine-induced dopamine release, and reduces nicotine self-administration. Varenicline is a clinically useful smoking cessation agent.
Coe et al (2005) Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 48(10) 3474 PMID: 15887955
Mihalak et al (2006) Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol. Pharmacol. 70 801 PMID: 16766716
Tonstad et al (2020) Varenicline: mode of action, efficacy, safety and accumulated experience salient for clinical populations. Curr Med Res Opin. 36(5) 713 PMID: 32050807
Related areas
All small molecules >
All nicotinic acetylcholine receptor modulators >
All neuroscience research categories >
Technical Data
| Structure | 7,8,9,10-Tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline tartrate:7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine tartrate |
| CAS Number | 375815-87-5 |
| Molecular Weight | 361.35 |
| Formula | C13H13N3·C4H6O6 |
Solubility and Storage
| Solubility | Soluble in DMSO to 18 mg/ml and water to 35 mg/ml |
| Appearance | Yellow solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >98% by HPLC, NMR conforms |
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