Antiemotional and anticonvulsant activity of brotizolam and its effects on motor performance in animals.
Brotizolam (2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-1,2,4-triazolo [4,3-a]-1,4-diazepine, We 941, Lendormin) is a thienotriazolo diazepine with predominantly sleep-inducing properties. Additionally, brotizolam, attenuated conflict behavior in rats and inhibited aggressive behavior in mice and cats. Brotizolam prevented audiogenic seizures in mice, seizures provoked by electroshock in rats and inhibited convulsions elicited by electrical stimulation in the limbic system of cats. Furthermore, brotizolam antagonized seizures induced by the convulsant drugs pentetrazol, bicuculline and strychnine in mice. Motocoordination was not impaired within the effective dose range. Muscle relaxant effects appeared at higher doses only. The onset of effect of brotizolam occurred in the different experiments within 15-30 min, thus indicating a fast enteral absorption and penetration of the blood-brain barrier. The duration of action within the therapeutic dose range was between 2-6 h. The effect of brotizolam was compared with other diazepine derivatives. Brotizolam was more active than diazepam, nitrazepam, estazolam, flurazepam and clonazepam and nearly as active as triazolam.
Böke-Kuhn
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Danneberg
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Kuhn
F J
FJ
Lehr
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D000161:Acoustic Stimulation; D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants; D001381:Azepines / Q000494:pharmacology*; D001569:Benzodiazepines; D002415:Cats; D003220:Conflict, Psychological; D004558:Electric Stimulation; D004644:Emotions / Q000187:drug effects*; D006993:Hypnotics and Sedatives / Q000494:pharmacology*; D007031:Hypothalamus / Q000502:physiology; D008032:Limbic System / Q000502:physiology; D051379:Mice; D008811:Mice, Inbred DBA; D011597:Psychomotor Performance / Q000187:drug effects*; D051381:Rats; D012934:Social Isolation; D013045:Species Specificity; D013997:Time Factors
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001381:Azepines; D006993:Hypnotics and Sedatives; D001569:Benzodiazepines; C020960:brotizolam