Rufinamide

Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na⁺ current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome^[1][2][3]. In Vitro:Rufinamide (10-300 μM) selectively binds to the slow-inactivated state (I_i) of Na⁺ channels in CHO-K1 and human embryonic kidney 293 cells transfected with human NaV 1.7 cDNA, causing a hyperpolarizing shift and a kinase-dependent block, and inhibits the resuscitation current in a dose-dependent manner^[1][3].
Rufinamide (100 µM) alleviates neuropathic pain in dorsal root ganglion neurons isolated from C57BL/6 mice by affecting the sodium ion stabilization inactivation effect^[3].
In Vivo:Rufinamide inhibits maximal electroshock-induced seizures in mice by intraperitoneal injection (ED₅₀: 15.5 mg/kg) and oral administration (ED₅₀: 23.9 mg/kg), in addition, intraperitoneal injection can also inhibit the clonus induced by pentylenetetrazol, Bicuculline (HY-N0219) and Picrotoxin (HY-101391) in mice (ED₅₀: 54.0, 50.5 and 76.3 mg/kg, respectively)^[2].
Rufinamide is non-neurotoxic and has a high protection index at doses that reduce seizures (i.p. TD₅₀: 500-1,000 mg/kg; p.o. TD₅₀: ≥ 1,000 mg/kg)^[2].
Rufinamide (p.o.) can effectively inhibit MES-induced seizures in Sprague-Dawley rats (ED₅₀: 6.1 mg/kg) and is well tolerated with low toxicity^[2].
Rufinamide (i.p., 5-50 mg/kg) dose-dependently alleviates neuropathic pain behaviors in the mouse spared nerve injury model without altering basal mechanical sensitivity or thermal paw withdrawal latency^[3].