Nakamura Y, Morimoto K, Moriwake T, Okamoto M, Sato K, Hirayasu Y, Katayama K, Onishi M, Otsuki S
Department of Neuropsychiatry, Okayama University Medical School, Japan.
Yakubutsu Seishin Kodo. 1989 Jun;9(2):241-4.
The anticonvulsant affects of bifemelane hydrochloride, a novel therapeutic drug for cerebrovascular dementia, were investigated in the kindling model of epilepsy in rats. The results obtained were as follows. (i) Both the seizure stage and afterdischarge duration of kindled seizures from the amygdala and hippocampus were significantly suppressed following systemic injection of bifemelane hydrochloride (5-30 mg/kg) in a dose-dependent manner. (ii) The efficacy of anticonvulsant action on kindled seizures from the hippocampus was more potent than from the amygdala. (iii) The maximum anticonvulsant effects were observed between 1 and 4 h after injection, and this time course was very similar to that of the previously reported increasing effects of bifemelane hydrochloride on noradrenaline levels in the rat brain. Thus, it is suggested that these anticonvulsant effects in kindling may be mediated by central noradrenergic systems. These results indicate that bifemelane hydrochloride has a potent anticonvulsant action on kindled seizures and may be useful for dementia patients with epilepsy or other seizure disorders.
研究了新型脑血管性痴呆治疗药物盐酸比芬美兰在大鼠癫痫点燃模型中的抗惊厥作用。所得结果如下：(i) 全身性注射盐酸比芬美兰（5 - 30毫克/千克）后，杏仁核和海马体点燃性癫痫发作的发作阶段和放电后持续时间均呈剂量依赖性显著抑制。(ii) 对海马体点燃性癫痫发作的抗惊厥作用效力比对杏仁核更强。(iii) 注射后1至4小时观察到最大抗惊厥效果，此时间进程与先前报道的盐酸比芬美兰对大鼠脑内去甲肾上腺素水平的增强作用非常相似。因此，提示点燃模型中的这些抗惊厥作用可能由中枢去甲肾上腺素能系统介导。这些结果表明，盐酸比芬美兰对点燃性癫痫发作具有强效抗惊厥作用，可能对患有癫痫或其他发作性疾病的痴呆患者有用。
