[Analgesic action and absence of physical dependence of 3-acetylaconitine].
[Analgesic action and absence of physical dependence of 3-acetylaconitine].
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发表时间：
1986-09
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通讯作者：
X. Tang;X. J. Liu;J. Feng;M. Zhu;A. Li
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作者：
X. Tang;X. J. Liu;J. Feng;M. Zhu;A. Li
本文采用腹腔注射0.7%醋酸10 ml/kg引起的小鼠扭体反应、热板上舔小鼠后爪反应、皮下注射2.5%甲醛0.03ml引起的小鼠前爪持续痛刺激反应和大鼠光刺激甩尾反应，研究了从中药黄花菜中提取的生物碱3-乙酰乌头碱（AAc）的镇痛作用。其镇痛作用的相对效价分别为吗啡和阿司匹林的5.1-35.6倍和1250-3912倍。纳洛酮不能拮抗醋酸钠的镇痛作用，而利血平3 mg/kg可在醋酸钠注射前3 h消除醋酸钠的镇痛作用。结果提示，AAc的镇痛作用可能与脑内单胺水平有关。AAc 0.25 mg/kg × 9 d热板每日皮下注射不能诱导吗啡耐受。在纳洛啡激发实验中，最大耐受剂量AAc 3.35mg/kg组小鼠无跳跃反应。单次给药抑制实验用于评估吗啡处理大鼠的AAc成瘾性，AAc 0.1mg/kg后体重变化与对照组无显著差异。3只猴皮下注射醋酸钠，bid，连续92-95 d，突然停药后及在第21、41、52、62、92 d用纳洛啡4 mg/kg激发后均未出现戒断症状。在2只吗啡依赖猴中，AAc不能抑制吗啡突然戒断或皮下注射纳洛啡0.5mg/kg引起的戒断症状。这些结果表明，AAc属于非麻醉性镇痛药。
The analgesic action of 3-acetylaconitine (AAc), an alkaloid isolated from Chinese herb Aconitum flavum, has been studied by the following methods; Mice writhing evoked by ip 0.7% acetic acid 10 ml/kg, mice licking hind paw on hot plate, continuous pain stimuli elicited by sc 2.5% formaldehyde 0.03 ml in fore paw of mice and rat tail-flick response to light irradiation. The relative potency of analgesic action of AAc was found to be 5.1-35.6 and 1250-3912 times that of morphin and aspirin, respectively. The analgesic action of AAc was not antagonized by naloxone, but was eliminated by ip reserpin 3 mg/kg 3 h prior to AAc. The results suggested that analgesic action of AAc may be related to the monoamine level in brain. Daily sc of AAc 0.25 mg/kg*9 d in mice with hot plate did not induce tolerance as seen with morphine. In nalorphine-challenged test, no jumping was seen in mice treated with AAc 3.35 mg/kg, the maximal tolerance dose. The single dose suppression test was applied to estimate addiction liability of AAc in morphine-treated rats, the change in body weight was not significantly different from that seen in the control after AAc 0.1 mg/kg. In 3 monkeys, AAc was injected sc bid for 92-95 d, no abstinence syndrome was seen after sudden AAc withdrawal or when challenged with nalorphine 4 mg/kg on d 21, 41, 52, 62, and 92, respectively. In 2 morphine-dependent monkeys, AAc did not suppress the abstinence syndrome evoked by sudden morphine withdrawal or by sc nalorphine 0.5 mg/kg. These results demonstrate that AAc belongs to the non-nacrotic analgesic.