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Varenicline dihydrochloride
- Chantix - Champix
- Parent CAS: 249296-44-4
- Soluble in water
- MF: C13H13N3.2HCl
- MW: 284.18
Description
Varenicline dihydrochloride is a high-affinity α4β2 nicotinic acetylcholine receptor partial agonist that provides submaximal receptor activation while competitively reducing nicotine-evoked signaling.
This dual agonist–antagonist profile supports smoking-cessation pharmacology by moderating withdrawal-related dopaminergic signaling and attenuating nicotine reinforcement. Varenicline is a clinically validated reference ligand for neuronal nicotinic receptor studies. Another drug form, Varenicline tartrate (Axon 2074), is also available.
Key Features
- α4β2 nicotinic receptor partial agonist
- Reduces nicotine-driven receptor activation
- Modulates mesolimbic dopamine release
- Clinically established smoking-cessation pharmacology
Applications
- α4β2 nAChR binding and functional assays
- Nicotine dependence and withdrawal research
- Mesolimbic reward-pathway studies
- Neuronal nicotinic receptor subtype profiling
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 dihydrochloride |
| extra_info | . |
| MFCD | MFCD12546330 |
| Short Description | α4β2 partial agonist |
References
- DE 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 (1), 56–63.
- RS 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.
- Mihalak K.B. et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-805.
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