Ueki S, Gomita Y, Ataki Y, Yamada K, Yoshimura H
Nihon Yakurigaku Zasshi. 1977 Mar;73(2):243-55. doi: 10.1254/fpj.73.243.
Effects on the central nervous system of ID-690, a new benzodiazepine derivative were investigated and compared mainly with those of diazepam in mice and rats. Locomotor activity of the rat was increased with ID-690, at doses of 2 approximately 5 mg/kg p.o., as with diazepam. ID-690 was approximately 5 times more potent than diazepam in inhibiting fighting behavior of long-term isolated mice. Hyperemotionality induced by either septal lesions or olfactory bulbectomy was also inhibited by ID-690. This effect was almost the same in potency as that of diazepam. ID-690 was only 1/30 as potent as diazepam in preventing maximal electroshock convulsion, while it was approximately 18 times more potent that diazepam in suppressing pentetrazol convulsion in mice. ID-690 was approximately 5 times as potent as diazepam in impairing rotarod performance in mice. The muscle relaxant effect of ID-690 was approximately 10 times as potent as diazepam, as measured with an inclined screen test in mice. Thus the effect of ID-690, as compared with diazepam, was characterized by its relatively potent muscle relaxant and extremely potent anti-pentetrazol convulsant action.
研究了新型苯二氮䓬衍生物ID - 690对中枢神经系统的作用,并主要在小鼠和大鼠中与地西泮的作用进行了比较。与地西泮一样,口服剂量为2至5mg/kg时,ID - 690可增加大鼠的运动活性。在抑制长期隔离小鼠的争斗行为方面,ID - 690的效力约为地西泮的5倍。ID - 690还可抑制由隔区损伤或嗅球切除引起的过度情绪反应。这种作用的效力与地西泮几乎相同。在预防最大电休克惊厥方面,ID - 690的效力仅为地西泮的1/30,而在抑制小鼠戊四氮惊厥方面,其效力约为地西泮的18倍。在损害小鼠转棒试验表现方面,ID - 690的效力约为地西泮的5倍。用小鼠倾斜筛试验测量,ID - 690的肌肉松弛作用效力约为地西泮的10倍。因此,与地西泮相比,ID - 690的作用特点是其具有相对较强的肌肉松弛作用和极强的抗戊四氮惊厥作用。