Nishino Tomomi, Takeuchi Tomoko, Takechi Kenshi, Kamei Chiaki
Department of Medicinal Pharmacology, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan.
J Pharmacol Sci. 2008 Jul;107(3):349-54. doi: 10.1254/jphs.08107fp. Epub 2008 Jul 5.
Anxiolytic-like effects of some short-acting benzodiazepine hypnotics were examined with experimental paradigms of anxiety using an elevated plus-maze in male ICR mice. Diazepam was used as a positive control. The drug at a dose of 1 mg/kg significantly increased the percentage of time spent in the open arms and percentage of the number of open arm entries in the elevated plus-maze. Triazolam, brotizolam, rilmazafone, and lormetazepam also showed an anxiolytic-like effect as indicated by the significant increase in the percentage of time spent in the open arms and percentage of the number of open arm entries. Effects of short-acting benzodiazepine hypnotics used in the study were more potent than those of diazepam. In addition, the doses affecting the elevated plus-maze by benzodiazepine hypnotics were much smaller than those that showed muscle-relaxant activity measured by the rotarod test, indicating that anxiolytic-like effects of benzodiazepine hypnotics had high specificity and selectivity.
使用高架十字迷宫焦虑实验范式,在雄性ICR小鼠中研究了一些短效苯二氮䓬类催眠药的抗焦虑样作用。地西泮用作阳性对照。剂量为1mg/kg的该药物显著增加了在高架十字迷宫中开放臂停留时间的百分比和进入开放臂次数的百分比。三唑仑、溴替唑仑、瑞马唑仑和氯美扎酮也表现出抗焦虑样作用,表现为开放臂停留时间百分比和进入开放臂次数百分比显著增加。研究中使用的短效苯二氮䓬类催眠药的作用比地西泮更强。此外,苯二氮䓬类催眠药影响高架十字迷宫的剂量远小于通过转棒试验测量显示肌肉松弛活性的剂量,表明苯二氮䓬类催眠药的抗焦虑样作用具有高特异性和选择性。