Pharmacological effects of triazolo[4,3-d] and tetrazolo[1,5-a][1,4]benzodiazepines on the central nervous system.
A series of tricyclic 1,4-benzodiazepines, fundamentally 5H-s-triazolo[4,3-d] and tetrazolo[1,5-a][1,4]benzodiazepines, were tested for acute toxicity and central nervous system effects in mice. All of these compounds, but especially 3, 4 and 5, showed a clear central depressant activity. Compounds 3, 4 and 5 also showed a moderate activity in antagonizing the deleterious effects produced by cardiazol but were ineffective in counteracting those elicited by strychnine. These same compounds 3, 4 and 5 presented a remarkable benzodiazepine-like action with a pharmacological profile similar to that of chlordiazepoxide.
Darias
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Departamento de Farmacología, Facultad de Farmacia, Universidad de La Laguna, Tenerife, Spain.
Abdala
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Martín-Herrera
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Vega
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D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D001831:Body Temperature / Q000187:drug effects; D005106:Exploratory Behavior / Q000187:drug effects; D005260:Female; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000494:pharmacology; D010424:Pentobarbital / Q000494:pharmacology; D012890:Sleep / Q000187:drug effects; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013997:Time Factors; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000927:Anticonvulsants; D006993:Hypnotics and Sedatives; D009125:Muscle Relaxants, Central; D013777:Tetrazoles; D014230:Triazoles; C408967:tetrazolo(1,5-a)(1,4)benzodiazepine; C408968:triazolo(4,3-d)benzodiazepine; D001569:Benzodiazepines; D010424:Pentobarbital