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Varenicline Hydrochloride
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 Hydrochloride图片
CAS NO:230615-23-3
包装与价格：
包装价格(元)
5mg询价
25mg询价

Varenicline Hydrochloride (CP 526555 hydrochloride) 是一种高亲和力、选择性的 α4β2 尼古丁乙酰胆碱受体 (nAChR) 部分激动剂和完整的 α7 nAChR 激动剂。
Cas No.230615-23-3
别名6,7,8,9-四氢-6,10-甲桥-6H-吡嗪并[2,3-H][3]苯并氮杂卓盐酸盐,CP 526555 hydrochloride
化学名(6R)-7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline hydrochloride
Canonical SMILESCl[H].[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C13H14ClN3
分子量247.72
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 Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist[1][2][3]. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM[4].

Varenicline (0.5-2 mg/kg/day; subcutaneous injection; twice daily; for 14 days; male Wistar rats) treatment shows a comparable significantly higher DRD2/3 availability in the ventral striatum of approximately 11%, while only the rats treated with 1 and 2 mg/kg/day dose shows significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively. Varenicline induces dose-dependent and sustained increases in striatal DRD2/3 in rats, particularly in the ventral striatum[1].

References:
[1]. Crunelle CL, et al. Dose-dependent and sustained effects of varenicline on dopamine D2/3 receptor availability in rats. Eur Neuropsychopharmacol. 2011 Feb;21(2):205-10.
[2]. Kikkawa H, et al. Single- and multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy Japanese adult smokers. J Clin Pharmacol. 2011 Apr;51(4):527-37.
[3]. Pachas GN, Cather C, Pratt SA et al. Varenicline for Smoking Cessation in Schizophrenia: Safety and Effectiveness in a 12-Week, Open-Label Trial. J Dual Diagn. 2012;8(2):117-125.
[4]. Bordia T, Hrachova M, Chin M et al. Varenicline Is a Potent Partial Agonist at α6β2* Nicotinic Acetylcholine Receptors in Rat and Monkey Striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34.

 
 
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