In mice, valrocemide affords complete protection against maximal electroshock-, pentylenetetrazole-, picrotoxin-, and bicuculline-induced seizures and 6-Hz “psychomotor” seizures with median effective dose (ED ₅₀ ) values of 151, 132, 275, 248, and 237 mg/kg, respectively. Valrocemide is also effective in preventing sound-induced seizures in Frings audiogenic-seizure susceptible mice (ED ₅₀ , 52 mg/kg). The median neurotoxic dose in mice is 332 mg/kg. After oral administration to rats, valrocemide is active in the MES test, with an ED ₅₀ of 73 mg/kg, and the median neurotoxic dose is 1,000 mg/kg. Intraperitoneal administration of 300 mg/kg of valrocemide to hippocampal kindled Sprague–Dawley rats block generalized seizures and shorten the afterdischarge duration significantly. Valrocemide also provides complete protection from focal seizures in the corneally kindled rats (ED ₅₀ , 161 mg/kg).