Varenicline Tartrate is a selective α7 and α4β2 nicotinic acetylcholine receptor (nAChR) agonist with an IC50 value of 250nM for α4β2 nAChR[1]. Varenicline Tartrate is a smoking cessation drug that can reduce nicotine dependence[2, 3].
In vitro, Varenicline Tartrate (1, 10, 100μM) treatment of human umbilical vein endothelial cells (HUVEC) for 24h reduced the expression of VE-cadherin in cells and promoted cell migration[4].
In vivo, Varenicline Tartrate (0.25-1.5mg/kg, 0.178-5.6mg/kg) was intraperitoneally injected into C57BL/6J and CD-1 mice, respectively, and showed antidepressant-like activity in the forced swimming test of mice, significantly reducing the immobility of both mice[5].
References:
[1] Magnus C J, Lee P H, Bonaventura J, et al. Ultrapotent chemogenetics for research and potential clinical applications[J]. Science, 2019, 364(6436): eaav5282.
[2] Fagerström K, Hughes J. Varenicline in the treatment of tobacco dependence[J]. Neuropsychiatric Disease and Treatment, 2008, 4(2): 353-363.
[3] Faessel H M, Obach R S, Rollema H, et al. A review of the clinical pharmacokinetics and pharmacodynamics of varenicline for smoking cessation[J]. Clinical pharmacokinetics, 2010, 49(12): 799-816.
[4] Koga M, Kanaoka Y, Sugiyama K, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor–mitogen activated protein kinase axis[J]. Toxicology, 2017, 390: 1-9.
[5] Rollema H, Guanowsky V, Mineur Y S, et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect[J]. European Journal of Pharmacology, 2009, 605(1-3): 114-116.
Varenicline Tartrate是一种选择性α7和α4β2烟碱型乙酰胆碱受体（nAChR）激动剂，对α4β2 nAChR的IC50值为250nM[1]。Varenicline Tartrate是一种戒烟药物，能够减少尼古丁依赖[2, 3]。
在体外，Varenicline Tartrate（1, 10, 100μM）处理人脐静脉内皮细胞（HUVEC）24h，降低了细胞中VE-钙粘蛋白的表达，促进了细胞迁移[4]。
在体内，Varenicline Tartrate（0.25-1.5mg/kg、0.178-5.6mg/kg）分别通过腹腔注射处理C57BL/6J、CD-1小鼠，在小鼠的强迫游泳实验中显示出抗抑郁样活性，显著减少了两种小鼠的静止状态[5]。