Behavioral Effects of Brotizolam, a New Thienotriazolodiazepine Derivative

Abstract

The behavioral effect of brotizolam was investigated in mice and rats, in comparison with those of diazepam, nitrazepam and estazolam. Locomotor activity of rats in an open field situation was slightly increased with smaller doses of brotizolam and estazolam and with larger doses of nitrazepam, while it was decreased with large doses of brotizolam and estazolam. The anticonflict effect of brotizolam in rats was approximately as potent as that of diazepam and was augmented following chronic administration for 10 days. In suppressing hyperemotionality and muricide of olfactory bulbectomized rats, brotizolam was more potent than diazepam, being approximately equipotent to nitrazepam and estazolam. Brotizolam, diazepam, nitrazepam and estazolam prevented both maximal electroshock and pentetrazol convulsions in mice, the effects on the latter being much more potent than those on the former. In impairing rotarod performance, brotizolam was as potent as estazolam and nitrazepam and was much more potentthan diazepam in mice, but was less potent than estazolam and nitrazepam in rats. These results indicate that brotizolam possesses pharmacological properties characteristic to benzodiazepines and that the activity is more potent than that of diazepam and approximately as potent as those of nitrazepam and estazolam.