Böke-Kuhn K, Danneberg P, Kuhn F J, Lehr E
Arzneimittelforschung. 1986 Mar;36(3A):528-31.
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.
溴替唑仑（2-溴-4-（2-氯苯基）-9-甲基-6H-噻吩并[3,2-f]-1,2,4-三唑并[4,3-a]-1,4-二氮杂卓，We 941，Lendormin）是一种噻吩并三唑二氮杂卓，主要具有诱导睡眠的特性。此外，溴替唑仑可减轻大鼠的冲突行为，并抑制小鼠和猫的攻击行为。溴替唑仑可预防小鼠的听源性惊厥、大鼠电休克诱发的惊厥，并抑制猫边缘系统电刺激引起的惊厥。此外，溴替唑仑可拮抗小鼠中由惊厥药物戊四氮、荷包牡丹碱和士的宁诱导的惊厥。在有效剂量范围内，运动协调功能未受损害。仅在较高剂量时才出现肌肉松弛作用。在不同实验中，溴替唑仑的起效时间在15 - 30分钟内，这表明其经肠道吸收迅速且能穿透血脑屏障。治疗剂量范围内的作用持续时间为2 - 6小时。将溴替唑仑的作用与其他二氮杂卓衍生物进行了比较。溴替唑仑比地西泮、硝西泮、艾司唑仑、氟西泮和氯硝西泮更具活性，且活性与三唑仑相近。
