| Bioactivity | Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and cytochrome P450 (CYP) 2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation[1][2][3]. | ||||||||||||
| Target | NMDA receptor; CYP450 2B; Cholinesterase (ChE) | ||||||||||||
| Invitro | Orphenadrine (30-300 μM) 表现出相对快速的浓度依赖性开放通道阻断动力学，Koff 为 0.013[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Orphenadrine 相关抗体: Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | 在 Orphenadrine 的促肿瘤作用研究中，对雄性大鼠做单次腹腔注射 N-二乙基亚硝胺 (DEN) 的预处理 2 周。Orphenadrine (0, 750, 1500 ppm; po; 6 wk) 加速肝细胞增殖，诱导肝脏肿瘤促进活性[2].Orphenadrine (30 mg/kg; po; 3 d) 可避免大鼠受 3-硝基丙酸 (3-NPA) (30 mg/kg; 3 d) 影响，而导致星形胶质细胞中神经元损伤标记物： [(3)H]-PK 11195 和 HSP27 的表达水平增加[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
| CAS | 83-98-7 | ||||||||||||
| Formula | C18H23NO | ||||||||||||
| Molar Mass | 269.38 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kornhuber J, et al. Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237-46. [2]. Morita R, et al. Liver tumor promoting effect of orphenadrine in rats and its possible mechanism of action including CAR activation and oxidative stress. J Toxicol Sci. 2013;38(3):403-13. [3]. Pubill D, et al. Orphenadrine prevents 3-nitropropionic acid-induced neurotoxicity in vitro and in vivo. Br J Pharmacol. 2001 Feb;132(3):693-702. |