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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
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
Varenicline (CP 526555) 是一种有效的 α4β2 烟碱乙酰胆碱受体 (nAChR) 部分激动剂,EC50 值为 2.3 μM。
Cas No.249296-44-4
别名伐尼克兰; CP 526555
化学名(6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline
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
分子式C13H13N3
分子量211.26
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.