3,15-二乙酰苯甲酰乌头原碱的镇痛作用、毒性及与其类似物的比较  

Analgesic effect and toxicity of 315-diacetyl- benzoylaconine and comparison with its analogues

作　　者：郑平[1] 杨煜荣[1] 张炜平[1] 王洪诚[2] 劳爱娜[2] 

机构地区：[1]包头医学院药理教研室 [2]中国科学院上海药物研究所

出　　处：《中国药理学报》1994年第3期239-243,共5页Acta Pharmacologica Sinica

摘　　要：3,15-二乙酰苯甲酰乌头原碱(Dia),3-乙酰乌头碱(Ace)和乌头碱(Aco)在五种疼痛模型上的治疗指数大小顺序均为Dia>Ace>Aco,给大鼠恒速iv时,Dia,Ace和Aco致心律失常剂量与其镇痛剂量的比分别为3.3,0.8和0.5,致呼吸抑制剂量与其镇痛剂量的比分别为3.9,0.5和0.3,三药的icv及sc ED_(50)比值及油水分布系数均为Dia和Ace大于Aco。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.

关 键 词：乌头 乌头碱 镇痛 心律失常 呼吸 

分 类 号：R965.2[医药卫生—药理学]