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Varenicline
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Varenicline图片
CAS NO:249296-44-4
规格:98%
分子量:211.26
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
α4β2 nAChRs antagonist
CAS:249296-44-4
分子式:C13H13N3
分子量:211.26
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[1] Garrison GD, Dugan SE. Varenicline: a first-line treatment option for smoking cessation. Clin Ther. 2009 Mar;31(3):463-91.