Kretzschmar R, Otto J, Teschendorf H J, Worstmann W
Arzneimittelforschung. 1976;26(6):1073-6.
The butyrophenone melperone (Eunerpan) in mice and rats caused a prominetn inhibition of spontaneous activity, whereas cataleptogenic and apomorphine-antagonistic properties were less pronounced. In rats the sleep-cycle was altered: decrease of wakefulness, increase of slow-wave sleep and a moderate reduction of rapid eye movement-(REM) sleep. In contrast to thioridazine and chlorpromazine the effect lasted only for 4 h, followed by a slight REM rebound. In rabbits melperone caused a decrease of muscle tone and with somewhat higher doses an inhibition of the arousal-reaction. As seen by the computerized spontaneous cortical EEG, dosages below 1 mg/kg caused a shift of the dominant frequency from theta- to delta-rhythm and an increase of power. Therefore the neuropharmacological pattern of the butyrophenone melperone is closely related to those of thioridazine or chlorpromazine, without, however, having their long action.
丁酰苯类药物美哌隆(Eunerpan)在小鼠和大鼠中可显著抑制自发活动,而其致僵和阿扑吗啡拮抗特性则不那么明显。在大鼠中,睡眠周期发生改变:觉醒减少、慢波睡眠增加以及快速眼动(REM)睡眠适度减少。与硫利达嗪和氯丙嗪不同,其作用仅持续4小时,随后有轻微的REM睡眠反弹。在兔子中,美哌隆可导致肌张力降低,剂量稍高时可抑制觉醒反应。从计算机化的自发皮层脑电图来看,低于1mg/kg的剂量会使优势频率从θ节律转变为δ节律,并增加功率。因此,丁酰苯类药物美哌隆的神经药理学模式与硫利达嗪或氯丙嗪密切相关,然而,它没有它们那样的长效作用。