Shika K, Nakata C, Ogura M, Tamada T, Fujimoto Y
Nihon Yakurigaku Zasshi. 1977 Oct;73(7):717-34. doi: 10.1254/fpj.73.717.
Effects of methyl o-(4-hydroxy-3-methoxycinnamoyl) reserpate (CD-3400) on the central nervous system in mice, rats and cats were investigated, and a comparison was made with such effects of reserpine and rescinamine. Inhibitory effects of CD-3400 on spontaneous motor activity and conditioned avoidance response were weaker and shorter than those of reserpine and rescinnamine. In the experiments of the inhibitory effects of the central actions such as ptosis, hypothermia, decrease in motor ability, potentiation of hexobarbital and taming, reserpine was found to be the most potent followed by rescinnamine and CD-3400, respectively. High doses of CD-3400 exhibited inhibitory effects on methamphetamine-induced hyperactivity in mice and this action was weaker than those of reserpine and rescinnamine. CD-3400, 80-160 mg/kg p.o., showed no significant effects on morphine-induced analgesia, while a slight inhibition was observed on the Straub-tail reaction using morphine. Reserpine, 0.5 mg/kg i.v., resulted in a drowsy pattern in the spontaneous EEG activity and the EEG arousal response was depressed, while with CD-3400, 5 mg/kg i.v., there was no drowsy pattern. CD-3400 as well as rescinnamine and reserpine remarkably depleted 5-HT levels in brain, heart and plasma and the potency of CD-3400, particularly in the brain, was weaker than the potency of reserpine and rescinnamine. These results indicate that CD-3400 is an antihypertensive agent with a low toxicity and a weak central action.
研究了邻甲氧基-(4-羟基-3-甲氧基肉桂酰)利血平(CD-3400)对小鼠、大鼠和猫中枢神经系统的作用,并与利血平和异利血胺的此类作用进行了比较。CD-3400对自发运动活动和条件性回避反应的抑制作用比利血平和异利血胺弱且持续时间短。在眼睑下垂、体温过低、运动能力下降、己巴比妥增强作用和驯服等中枢作用的抑制实验中,发现利血平作用最强,其次分别是异利血胺和CD-3400。高剂量的CD-3400对小鼠甲基苯丙胺诱导的多动有抑制作用,且该作用比利血平和异利血胺弱。口服80-160mg/kg的CD-3400对吗啡诱导的镇痛无显著影响,而在使用吗啡的斯特劳布尾反应中观察到轻微抑制。静脉注射0.5mg/kg的利血平导致自发脑电图活动出现嗜睡模式,脑电图觉醒反应受到抑制,而静脉注射5mg/kg的CD-3400则无嗜睡模式。CD-3400以及异利血胺和利血平显著降低了脑、心脏和血浆中的5-羟色胺水平,且CD-3400的效力,尤其是在脑中,比利血平和异利血胺弱。这些结果表明,CD-3400是一种毒性低、中枢作用弱的抗高血压药物。