title: Anticonvulsant activity in photosensitive baboons, Papio papio, of two new 1,5 benzodiazepines.
abstract: 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.
mesh_terms: D000818:Animals; D000927:Anticonvulsants; D001569:Benzodiazepines / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005260:Female; D000882:Haplorhini; D006993:Hypnotics and Sedatives / Q000494:pharmacology; D009129:Muscle Tonus / Q000187:drug effects; D010215:Papio; D010775:Photic Stimulation; D010787:Photosensitivity Disorders / Q000150:complications*; D012640:Seizures / Q000209:etiology / Q000517:prevention & control; D013997:Time Factors
chemical_list: D000927:Anticonvulsants; D006993:Hypnotics and Sedatives; D001569:Benzodiazepines