Ueki S, Watanabe S, Fujiwara M, Yamamoto T, Araki H, Ohmori K
Nihon Yakurigaku Zasshi. 1978 Jul;74(5):597-614. doi: 10.1254/fpj.74.597.
Triazolam was 4 to 5 times as potent as diazepam in reducing hyperemotionality of either septal-lesioned or olfactory bulbectomized rats (O.B. rats), and in suppressing muricide in O.B. rats. This agent was equipotent with diazepam in inhibiting fighting behavior of long-term isolated mice, but was longer in duration of action. Triazolam was approximately 4 times more potent than diazepam in preventing pentetrazol convulsion, but was 10 times less potent in inhibiting maximal electroshock convulsion in mice. The muscle relaxant effect of triazolam as assessed by the inclined screen test was 34 times, and the effect on rotarod performance was 17 times more potent than that of diazepam in mice. Triazolam (0.2 approximately 0.5 mg/kg i.v.) changed the EEG to a drowsy pattern in unanesthetized rabbits with a chronic electrode implant, and suppressed the EEG arousal response to auditory stimulation and electrical stimulation given to either the mesencephalic reticular formation or posterior hypothalamus. The limbic afterdischarges induced by either hippocampal or amygdaloid stimulation were also markedly inhibited by triazolam. These EEG effects of triazolam were qualitatively similar to, but were 4 to 5 times more potent than those of diazepam. These results indicate that triazolam is a potent tranquilizer with a longer duration of action, and the muscle relaxant effect is considerable as compared with diazepam.
三唑仑在减轻隔区损伤或嗅球切除大鼠（O.B.大鼠）的过度情绪反应以及抑制O.B.大鼠的杀鼠行为方面，效力是地西泮的4至5倍。在抑制长期隔离小鼠的打斗行为方面，该药物与地西泮效力相当，但作用持续时间更长。在预防戊四氮惊厥方面，三唑仑的效力约为地西泮的4倍，但在抑制小鼠最大电休克惊厥方面，效力比地西泮低10倍。通过倾斜屏幕试验评估，三唑仑对小鼠的肌肉松弛作用是地西泮的34倍，对转棒试验表现的作用效力是地西泮的17倍。三唑仑（静脉注射0.2至0.5毫克/千克）可使植入慢性电极的未麻醉家兔脑电图转变为嗜睡模式，并抑制脑电图对听觉刺激以及给予中脑网状结构或下丘脑后部的电刺激的觉醒反应。海马或杏仁核刺激诱发的边缘性后放电也被三唑仑显著抑制。三唑仑的这些脑电图效应在性质上与地西泮相似，但效力比地西泮强4至5倍。这些结果表明，三唑仑是一种效力强大且作用持续时间更长的镇静剂，与地西泮相比，其肌肉松弛作用相当可观。
