Varenicline
Varenicline is a partial agonist/antagonist of α4β2 nicotinic acetylcholine receptor [1].
Varenicline is a manufactured tartrate salt, it is a partial agonist of α4β2 nAChRs. The affinity(0.15 nM) of varenicline with α4β2 nAChRs is much more higher than with other nAChR subtypes. Through the binding, varenicline prevents nicotine from occupying the receptors and subsequently inhibit nicotine-induced dopaminergic activation. So varenicline is used for smoking cessation. In healthy adult smokers, varenicline does not undergo significant hepatic metabolism and the clearance(>90%) is predominantly renal. It is shown that the amphetamine administration may have decrease the efficacy of varenicline [1].
References:
[1] Garrison GD, Dugan SE. Varenicline: a first-line treatment option for smoking cessation. Clin Ther. 2009 Mar;31(3):463-91.
| Storage | Store at -20°C |
| M.Wt | 211.26 |
| Cas No. | 249296-44-4 |
| Formula | C13H13N3 |
| Solubility | Soluble in DMSO |
| Chemical Name | (6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline |
| SDF | Download SDF |
| Canonical SMILES | [H]C1(C([H])([H])N([H])C2([H])[H])C([H])([H])[C@]2([H])C3=C([H])C4=NC([H])=C([H])N=C4C([H])=C13 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
