Rufinamide (E 2080; CGP 33101; RUF 331) 是一种新型抗癫痫药物，在结构上不同于其他抗癫痫药物，被批准作为 Lennox-Gastaut 综合征 (LGS) 的辅助治疗药物。
| Cas No. | 106308-44-5 |
| 别名 | 卢非酰胺; CGP 33101; E 2080; RUF 331 |
| 化学名 | 1-[(2,6-difluorophenyl)methyl]triazole-4-carboxamide |
| Canonical SMILES | C1=CC(=C(C(=C1)F)CN2C=C(N=N2)C(=O)N)F |
| 分子式 | C10H8F2N4O |
| 分子量 | 238.19 |
| 溶解度 | ≥ 11.25mg/mL in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Rufinamide(E 2080; CGP 33101; RUF 331) is a new antiepileptic agent that differs structurally from other antiepileptic drugs and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS).IC50 Value:Target: in vitro:in vivo: Rufinamide and amitriptyline alleviated injury-induced mechanical allodynia for 4 h (maximal effect: 0.10 ± 0.03 g (mean ± SD) to 1.99 ± 0.26 g for rufinamide and 0.25 ± 0.22 g to 1.92 ± 0.85 g for amitriptyline) in mice [1]. Oral rufinamide suppressed pentylenetetrazol-induced seizures in mice (ED(50) 45.8 mg/kg) but not rats, and was active against MES-induced tonic seizures in mice (ED(50) 23.9 mg/kg) and rats (ED(50) 6.1 mg/kg) [2]. Intraperitoneal rufinamide suppressed pentylenetetrazol-, bicuculline-, and picrotoxin-induced clonus in mice (ED(50) 54.0, 50.5, and 76.3 mg/kg, respectively).Clinical trial: Exploratory Study to Evaluate the Effect of SYN-111 (Rufinamide) in Patients With Generalized Anxiety Disorder (GAD). Phase 2 References:
[1]. Suter MR, Kirschmann G, Laedermann CJ, Rufinamide attenuates mechanical allodynia in a model of neuropathic pain in the mouse and stabilizes voltage-gated sodium channel inactivated state. Anesthesiology. 2013 Jan;118(1):160-72.
[2]. White HS, Franklin MR, Kupferberg HJ, The anticonvulsant profile of rufinamide (CGP 33101) in rodent seizure models. Epilepsia. 2008 Jul;49(7):1213-20. |
