Tizanidine是一种口服有效的中枢性α2-肾上腺素能受体激动剂，通过抑制脊髓兴奋性氨基酸释放发挥骨骼肌松弛作用。该化合物具有抗伤害效应与胃肠道转运抑制作用，并能通过调控Nischarin-AKT及Wnt3a/β-catenin信号通路抑制肺癌细胞增殖迁移并诱导凋亡，临床用于多发性硬化、中风及脊髓损伤所致的痉挛治疗。
| 英文别名 (English Synonym) | Tizanidine |
| 中文名称 (Chinese Name) | 替扎尼定 |
| 靶点 (Target) | Adrenergic Receptor |
| 通路 (Pathway) | GPCR/G protein |
| CAS号 (CAS NO.) | 51322-75-9 |
| 分子式 (Formula) | C9H8ClN5S |
| 分子量 (Molecular Weight) | 253.71 |
| 纯度 (Purity) | ≥98% |
| 溶解性 (Solubility) | 溶于DMSO |
-25~-15℃保存，有效期3年
[1] Granfors MT, Backman JT, Laitila J, Neuvonen PJ. Tizanidine is mainly metabolized by cytochrome p450 1A2 in vitro. Br J Clin Pharmacol. 2004 Mar;57(3):349-53. doi: 10.1046/j.1365-2125.2003.02028.x. PMID: 14998432; PMCID: PMC1884447.[2]Zhao L, Zhao G, Xue Q. Tizanidine (Hydrochloride) Inhibits A549 Lung Cancer Cell Proliferation and Motility Through Regulating Nischarin. Onco Targets Ther. 2020 Jan 10;13:291-298. doi: 10.2147/OTT.S228317. PMID: 32021275; PMCID: PMC6966956.[3]Rodríguez-Palma EJ, Castelo-Flores DG, Caram-Salas NL, Salinas-Abarca AB, Centurión D, De la Luz-Cuellar YE, Granados-Soto V. Sex-dependent antiallodynic effect of α2 adrenergic receptor agonist tizanidine in rats with experimental neuropathic pain. Eur J Pharmacol. 2022 Apr 5;920:174855. doi: 10.1016/j.ejphar.2022.174855. Epub 2022 Feb 25. PMID: 35227682.
