Gomita Y, Ichimaru Y, Moriyama M, Fukamachi K, Uchikado A, Araki Y, Fukuda T, Koyama T
Nihon Yakurigaku Zasshi. 1981 Mar;77(3):245-59.
Coixol (6-methoxybenzoxazolone) contained in Coix Lachryma-Jobi L. var. ma-yuen Stapf was compared with chlorzoxazone with respect to behavioral and EEG effects in mice and rats. Coixol 50-100 mg/kg, i.p. decreased locomotor activities of both species and produced hypothermia in rats. These effects of coixol were the same in potency as chlorzoxazone given in the same dose. Coixol was approximately twice as potent as chlorzoxazone in potentiating thiopental-induced sleep. This compound attenuated the writhing syndrome induced by 1% acetic acid and increased the threshold to jumping response induced by foot shock, to the same degree as seen with chlorzoxazone. Coixol was equipotent to chlorzoxazone in preventing convulsions induced by maximal electro-shock, while it was about 1.5 times more potent than chlorzoxazone in suppressing pentylenetetrazol-induced convulsion. Coixol 20-100 mg/kg inhibited the lever pressing response of hypothalamic self-stimulation in rats. In rats with chronically implanted electrodes, coixol 50-100 mg/kg induced drowsy patterns on the spontaneous EEG. The EEG arousal response to the external auditory stimulation was inhibited by the same doses of coixol, whereas it failed to suppress the arousal response to the midbrain reticular stimulation. These results indicate that coixol has pharmacological properties qualitatively similar to chlorzoxazone and acts as a central muscle relaxant with an anti-convulsant effect.
对薏苡仁变种元米中所含的薏苡仁素（6-甲氧基苯并恶唑酮）与氯唑沙宗在小鼠和大鼠身上的行为及脑电图效应进行了比较。腹腔注射50-100mg/kg的薏苡仁素可降低两种动物的自发活动，并使大鼠体温降低。薏苡仁素的这些效应在强度上与相同剂量的氯唑沙宗相同。在增强硫喷妥钠诱导的睡眠方面，薏苡仁素的效力约为氯唑沙宗的两倍。该化合物减轻了1%醋酸诱导的扭体综合征，并提高了足部电击诱导的跳跃反应阈值，其程度与氯唑沙宗相同。在预防最大电休克诱导的惊厥方面，薏苡仁素与氯唑沙宗等效，而在抑制戊四氮诱导的惊厥方面，其效力比氯唑沙宗高约1.5倍。20-100mg/kg的薏苡仁素可抑制大鼠下丘脑自我刺激的杠杆按压反应。在长期植入电极的大鼠中，50-100mg/kg的薏苡仁素可在自发脑电图上诱导出嗜睡模式。相同剂量的薏苡仁素可抑制对外部听觉刺激的脑电图觉醒反应，而它不能抑制对中脑网状刺激的觉醒反应。这些结果表明，薏苡仁素具有与氯唑沙宗性质相似的药理特性，可作为一种具有抗惊厥作用的中枢性肌肉松弛剂。
