Zheng P, Yang Y R, Zhang W P, Wang H C, Lao A N
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai.
Zhongguo Yao Li Xue Bao. 1994 May;15(3):239-43.
3, 15-Diacetylbenzoylaconine (Dia) is a new aconite alkaloid derivative. The analgesic ED50 (95% confidence limit) of sc Dia measured with the HAc-induced writhing method, hot-plate method and electric stimulation method in mice were 2.76 (2.34-3.26), 3.50 (2.69-4.54), and 4.20 (3.72-4.73) mg.kg-1, respectively. With the hot-plate method and tail flick method in rats, the analgesic ED50 of ip Dia were 2.75 (2.28-3.31) and 5.24 (4.35-6.31) mg.kg-1, respectively. The LD50 of sc Dia in mice and ip Dia in rats were 21.68 (17.25-27.25) and 10.96 (8.24-14.56) mg.kg-1, respectively. The magnitude of the analgesic therapeutic indices of Dia, 3-acetylaconitine (Ace) and aconitine (Aco) in all the above-mentioned algo-model were in the order of Dia > Ace > Aco. When they were injected iv at 0.1 ml.min-1 in rats, the doses of Dia, Ace, and Aco producing arrythmia were 3.3, 0.8, and 0.5 times as large as those producing analgesia while those of Dia, Ace, and Aco inducing respiratory inhibition were 3.9, 0.5 and 0.3 times, respectively. The magnitudes of the oil/water distribution coefficients with two method and the quotient ED50 icv/ED50 sc of Dia and Ace were > Aco.
3,15 - 二乙酰苯甲酰乌头原碱（Dia）是一种新的乌头生物碱衍生物。采用醋酸诱导扭体法、热板法和电刺激法在小鼠中测得的皮下注射Dia的镇痛ED50（95%置信限）分别为2.76（2.34 - 3.26）、3.50（2.69 - 4.54）和4.20（3.72 - 4.73）mg·kg⁻¹。采用热板法和甩尾法在大鼠中测得的腹腔注射Dia的镇痛ED50分别为2.75（2.28 - 3.31）和5.24（4.35 - 6.31）mg·kg⁻¹。小鼠皮下注射Dia和大鼠腹腔注射Dia的LD50分别为21.68（17.25 - 27.25）和10.96（8.24 - 14.56）mg·kg⁻¹。在上述所有镇痛模型中，Dia、3 - 乙酰乌头碱（Ace）和乌头碱（Aco）的镇痛治疗指数大小顺序为Dia > Ace > Aco。当它们以0.1 ml·min⁻¹的速度静脉注射到大鼠体内时，产生心律失常的Dia、Ace和Aco的剂量分别是产生镇痛作用剂量的3.3、0.8和0.5倍，而诱导呼吸抑制的Dia、Ace和Aco的剂量分别是3.9、0.5和0.3倍。Dia和Ace的两种方法的油/水分配系数大小以及脑室内注射ED50与皮下注射ED50的比值均大于Aco。
