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Varenicline tartrate
- Chantix - Champix - CP 526555-18
- Parent CAS: 249296-44-4
- Optical Purity: Optically pure
- Soluble in water and DMSO
- MF: C13H13N3.C4H6O6
- MW: 361.35
Description
Varenicline tartrate is a selective α4β2 nicotinic acetylcholine receptor partial agonist. It provides partial receptor activation while reducing nicotine-driven reinforcement through competitive occupancy of α4β2 nAChRs.
α4β2 nicotinic receptors regulate mesolimbic dopamine release, reward circuitry and nicotine dependence. Varenicline is useful for studying nicotinic partial agonism, addiction pharmacology and smoking-cessation mechanisms.
Key Features
- Selective α4β2 nAChR partial agonist
- Modulates nicotine-responsive reward signaling
- Competitive functional profile at nicotinic receptors
- Relevant to addiction and smoking-cessation research
Applications
- α4β2 nAChR binding assays
- Nicotine dependence models
- Dopamine reward pathway studies
- Partial agonist pharmacology profiling
Related information: Varenicline dihydrochloride is available as Axon 1384.
More Information
| Parent CAS No. | 249296-44-4 |
|---|---|
| Chemical Name | 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine tartrate |
| extra_info | . |
| SMILES | C1N=C2C=C3[C@H]4CNC[C@H](C4)C3=CC2=NC=1.C(O)(=O)[C@@H]([C@H](C(O)=O)O)O |&1:5,9,19,20,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C13H13N3.C4H6O6/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;5-1(3(7)8)2(6)4(9)10/h1-2,4-5,8-9,14H,3,6-7H2;1-2,5-6H,(H,7,8)(H,9,10)/t8-,9+;1-,2-/m.1/s1 |
| InChiKey | TWYFGYXQSYOKLK-CYUSMAIQSA-N |
| CID | 6918678 |
| Short Description | α4β2 partial agonist |
References
- D.E. Jorenby et al. Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA 2006, 296, 56-63.
- R.S. Obach et al. Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab. Dispos. 2006, 34, 121-30.
- K.B. Mihalak et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol. Pharmacol. 2006, 70, 801-805.
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