ANTICONVULSANT ACTIVITY IN PHOTOSENSITIVE BABOONS, PAPIO-PAPIO, OF 2 NEW 1,5 BENZODIAZEPINES

Two new 1,5 benzodiazepines have been evaluated acutely as anticonvulsants in baboons, Papio papio, with photosensitive epilepsy. BAU 426 (8-Chlor-6-[2-chlorphenyl]-4H-s-triazolo-[4,3-a] [1,5-benzodiazepin-5-[6-H]on) and BAU 500 (analogue of BAU 426 with [2-trifluor methylphenyl] substituted for [2-chlorphenyl]), 0.1-5.0 mg/kg, were administered i.v. to baboons with and without priming with D,l allylglycine. BAU 426 or BAU 500, 0.1-0.2 mg/kg, produced partial or transient protection against photically induced myoclonus or epileptic responses. Complete protection, in the absence of signs of sedation or acute neurological toxicity, was seen 1-4 h after 0.5-2 mg/kg. EEG changes typical of benzodiazepines were seen for 1-3 h and clinical signs of sedation with some muscular hypotonia were evident for 1 h after either drug, 5 mg/kg. Clinical trials are required to determine if these compounds are superior to 1,4 benzodiazepines as anticonvulsants. © 1979 Springer-Verlag.