Varenicline Tartrate是一种口服有效的α4β2烟碱乙酰胆碱受体部分激动剂,同时作为α6β2 nAChR部分激动剂及α6β2 nAChR完全激动剂;该药物通过阻断尼古丁对nAChR的直接激动作用并温和激活受体,广泛用于辅助戒烟治疗。
| 英文别名 (English Synonym) | Varenicline Tartrate |
| 中文名称 (Chinese Name) | 酒石酸伐尼克兰 |
| 靶点 (Target) | AChR |
| 通路 (Pathway) | Neuroscience |
| CAS号 (CAS NO.) | 375815-87-5 |
| 分子式 (Formula) | C13H13N3·C4H6O6 |
| 分子量 (Molecular Weight) | 361.35 |
| 纯度 (Purity) | ≥98% |
| 溶解性 (Solubility) | 溶于DMSO |
-25~-15℃保存,有效期3年
[1] Koga M, Kanaoka Y, Sugiyama K, Ohishi K, Ejima Y, Hisanaga M, Kataoka Y, Yamauchi A. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017 Sep 1;390:1-9. doi: 10.1016/j.tox.2017.08.006. Epub 2017 Aug 24. PMID: 28842382.
[2] Ren J, Ding X, Greer JJ. Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Anesthesiology. 2020 May;132(5):1197-1211. doi: 10.1097/ALN.0000000000003128. PMID: 32294065.





