[Analgesic actions and local anesthetic activity of 3-acetylaconitine hydrobromide (author's transl)].
[Analgesic actions and local anesthetic activity of 3-acetylaconitine hydrobromide (author's transl)].
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发表时间：
1981-06
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通讯作者：
X. Tang;J. Feng
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作者：
X. Tang;J. Feng
3-乙酰乌头碱为首次从黄药子和乌头根中分离得到。钟摆。本文研究了氢溴酸3-乙酰乌头碱的镇痛和局麻活性。小鼠皮下注射0.7%醋酸热板法和牵拉法的半数镇痛量（ED_（50））分别为0.21和0.13mg/kg。其镇痛作用强于乌头碱。3-乙酰乌头碱具有较弱的角膜麻醉活性。对小鼠坐骨神经阻滞和豚鼠皮内风团试验的麻醉活性分别为可卡因的92倍和53倍。小鼠sc LD_（50）为1.4mg/kg，急性毒性低于乌头碱。因此，3-乙酰乌头碱的治疗指数高于乌头碱。
3-Acetylaconitine was first isolated from the root of Aconitum flavum and A. pendulum. The analgesic and local anesthetic activity of 3-acetylaconitine hydrobromide were studied in this paper. The sc median analgesic dose (ED50) in mice were 0.21 and 0.13 mg/kg, respectively, with the hot plate and stretching method induced by ip 0.7% acetic acid. Its analgesic action was stronger than that of aconitine. 3-Acetylaconitine possessed a weak corneal anesthetic activity. Its local anesthetic activities on sciatic nerve block in mice and intracutaneous wheal test in guinea pig were found to be 92 and 53 times, respectively, as active as cocaine. The sc LD50 of 3-acetylaconitine was 1.4 mg/kg in mice, its acute toxicity was lower than that of aconitine. So 3-acetylaconitine exhibited a higher therapeutic index than aconitine.