Background:

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

参考文献:
[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.