Sato M
Nihon Yakurigaku Zasshi. 1979 Oct;75(7):695-706.
M73101 decreased spontaneous locomotor activity in both mice and rats and prolonged sleeping time induced by hexobarbital in mice. There was no evidence of cataleptogenic action, anti-tremorine action and antagonistic effect on reserpine-induced hypothermia in mice. M73101 did not inhibit convulsions induced by maximal electroshock and pentylenetetrazol but slightly inhibited the convulsion induced by strychnine in mice. Moreover, M73101 depressed only the monosynaptic action potential in intact and spinal cats, indicating that this compound exerts an inhibitory action on spinal function. On the EEG of rabbits, M73101 produced an arousal pattern in the spontaneous EEG and inhibited the recruiting response, but had no marked influence on the EEG arousal response, augmenting response and hippocampal afterdischarge. The arousal pattern in the spontaneous EEG induced by M73101 and the inhibitory action of this compound on the recruiting response were absent in the cerveau isolé preparation of the rabbit, indicating that M73101 may stimulate the brainstem reticular formation and that the inhibition of recruiting response may be related to the stimulatory effect. These properties of M73101 on the central nervous system are similar to those seen with aminopyrine though the potency was weaker. M73101 like aminopyrine showed no marked activity on the motor function.
M73101可降低小鼠和大鼠的自发运动活性,并延长小鼠由己巴比妥诱导的睡眠时间。没有证据表明M73101对小鼠有引起僵住症的作用、抗震颤素作用以及对利血平诱导的体温过低的拮抗作用。M73101不抑制最大电休克和戊四氮诱导的惊厥,但略微抑制士的宁诱导的小鼠惊厥。此外,M73101仅抑制完整和脊髓猫的单突触动作电位,表明该化合物对脊髓功能发挥抑制作用。在兔脑电图上,M73101在自发脑电图中产生觉醒模式并抑制募集反应,但对脑电图觉醒反应、增强反应和海马后放电没有明显影响。在兔孤立脑制备中,M73101诱导的自发脑电图觉醒模式以及该化合物对募集反应的抑制作用不存在,这表明M73101可能刺激脑干网状结构,并且募集反应的抑制可能与刺激作用有关。M73101对中枢神经系统的这些特性与氨基比林相似,尽管效力较弱。M73101与氨基比林一样,对运动功能没有明显活性。