唐希灿, 朱梅英, 冯洁, 王月娥. 刺乌头碱氢溴酸盐的药理作用研究J. 药学学报, 1983, 18(8): 579-584.
引用本文: 唐希灿, 朱梅英, 冯洁, 王月娥. 刺乌头碱氢溴酸盐的药理作用研究J. 药学学报, 1983, 18(8): 579-584.
TANG Xi-can, ZHU Mei-ying, FENG Jie , WANG Yue-e, . STUDIES ON PHARMACOLOGIC ACTIONS OF LAPPACONITINE HYDROBROMIDEJ. Acta Pharmaceutica Sinica, 1983, 18(8): 579-584.
Citation: TANG Xi-can, ZHU Mei-ying, FENG Jie , WANG Yue-e, . STUDIES ON PHARMACOLOGIC ACTIONS OF LAPPACONITINE HYDROBROMIDEJ. Acta Pharmaceutica Sinica, 1983, 18(8): 579-584.

刺乌头碱氢溴酸盐的药理作用研究

STUDIES ON PHARMACOLOGIC ACTIONS OF LAPPACONITINE HYDROBROMIDE

  • 摘要: 用热板,扭体反应(小鼠)和光热甩尾法测试表明,刺乌头碱均有镇痛作用。小鼠多次注射刺乌头碱后,再给予烯丙吗啡,不出现跳跃反应。对依赖吗啡大鼠或猴停药后的戒断症状无替代取消作用。猴长期注射刺乌头碱后停药不出现戒断综合症,表明刺乌头碱是一种不成瘾的止痛剂。刺乌头碱有较强的局部麻醉作用。对三联疫苗发热小鼠有解热作用。对大鼠甲醛性“关节炎”有消炎作用。

     

    Abstract: Lappaconitin e was isolated from the root of Aconitum sinomantanum Nakai which has been used as an anodyne in the northwestern part of China. In this paper, the analgesic effects of lappaconitine were demonstrated by using the mice hot plate method and the rat tail-flick test after intraperitoneal injection of 6 mg/kg. Assayed with the writhing method, the median analgesic dose (ED50) of lappaconitine in mice was found tO be 3.5 mg/kg. In the 2-day test(8), no jumping was observed in mice treated with lappaconitine and then challenged with nalorphine. The single dose suppression test was applied to estimate addiction liability of lappaconitine in morphine-treated rats, the change in body weightwas not significantly different from that seen in the control after given lappaconitine at doses of 8 mg/kg. In three morphine-dependent monkeys, lappaconitine at doses of 2 mg/kg, which was the maximal tolerated dose, did not suppress the withdrawal symptoms evoked by sudden morphine withdrawal or by subcutaneous injection of nalorphine (0.5 mg/kg). In three monkeys, lappaconitine were administrated for 53-92 days, and the physical dependence was determined. During this period no physical dependence was observed. No withdrawal symptoms were observed when challenged with nalorphine at doses of 4-8 mg/kg.Anaesthesia test on rabbit cornea showed that the surface anaesthetic potency of lappaconitine was eight times stronger than that of cocaine. Its local anesthetic activities on sciatic nerve block in mice and intracutaneous wheal test in guinea pig were found to be 5 times and about the same, respectively, as active as cocaine.Iappaconitine was shown to have antithermic effect in normothermic and pyrexial mice after intraperitoneal injection of 3 mg/kg. In rats, after intraperitoneal injection lappaconitine 4 mg/kg qd × 7 days, a marked reduction in formaldehydeinduced edema of the hind paw was noted.

     

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