Mitsushima T, Ueki S
Nihon Yakurigaku Zasshi. 1978 Nov;74(8):959-79. doi: 10.1254/fpj.74.959.
Behavioral effects of Flutazolam (MS-4101), a new derivative of benzodiazepines, was investigated and compared with effects of diazepam in mice and rats. MS-4101 suppressed hyperemotionality in septal rats, fighting behavior in long-term isolated mice and pentylenetetrazol convulsion and potentiated thiopental sleep. These effects of MS-4101 were the same in potency as those of diazepam. MS-4101 was more potent than diazepam in reducing the spontaneous locomotor activity in the open-field test and potentiating the stimulant effect of methamphetamine on locomotor activity. On the other hand, suppression of hyperemotionality in O. B. rats, potentiation of ethanol-induced anesthesia, prevention of maximal electroshock, prevention of strychnine convulsin and muscle relaxant effect of MS-4101 were less potent than in the case of diazepam. MS-4101 had also an anticonflict effect, which was less potent than that seen with diazepam. Suppression of locomotor activity was potentiated by chronic administration of MS-4101, but disappeared with chronic administration of diazepam. MS-4101 inhibited considerably both scratching and head-twitch induced by mescaline in mice. Scratching was increased with small doses of diazepam and decreased with high doses. Head-twitch was decreased with small doses of diazepam and increased with high doses.
研究了苯二氮䓬类新衍生物氟他唑仑(MS - 4101)的行为效应,并与地西泮对小鼠和大鼠的效应进行了比较。MS - 4101可抑制隔区大鼠的过度情绪反应、长期隔离小鼠的打斗行为以及戊四氮惊厥,并增强硫喷妥钠诱导的睡眠。MS - 4101的这些效应在效力上与地西泮相同。在旷场试验中,MS - 4101在降低自发运动活性和增强甲基苯丙胺对运动活性的兴奋作用方面比地西泮更有效。另一方面,MS - 4101对肥胖大鼠过度情绪反应的抑制、乙醇诱导麻醉的增强、最大电休克的预防、士的宁惊厥的预防以及肌肉松弛作用,其效力均低于地西泮。MS - 4101也有抗冲突效应,但其效力低于地西泮。长期给予MS - 4101可增强对运动活性的抑制,但长期给予地西泮则这种抑制消失。MS - 4101可显著抑制小鼠中由三甲氧苯乙胺诱导的抓挠和头部抽搐。小剂量地西泮可增加抓挠,大剂量则减少抓挠。小剂量地西泮可减少头部抽搐,大剂量则增加头部抽搐。