论文部分内容阅读
依托尼秦(eton itazene,旧称苯咪胺)是最早人工合成的高效镇痛剂,其镇痛活性在小鼠高于吗啡1000倍以上,但由于其具有较强的呼吸抑制作用而未能在临床应用。我们将其-CH_2 -CH_2N(C_2H_5)_2基团改造为-CH_2CH_2N基团,代号B_(8901)。实验表明B_(8901)具有与依托尼秦相当的镇痛活性,但有效作用时间延长约30 min,本实验探讨了依托尼秦和B_(8901)对小鼠、大鼠致依赖性的特点。由于依托尼秦和B_(8901)的有效作用时间均在90 min以内,少于吗啡的一半,采用每天4次给药,吗啡为每天给药2次。在小鼠,采用跳跃实验,结果为:等效镇痛剂量递增
Eton itazene (formerly known as cimetidine) is the earliest synthetic highly effective analgesic, its analgesic activity in mice than 1000 times higher than morphine, but because of its strong respiratory depression and failed to Clinical application. We transform its -CH_2 -CH_2N (C_2H_5) _2 group into -CH_2CH_2N group, code B_ (8901). Experiments show that B_ (8901) has the same analgesic activity as etomidate, but the effective action time is extended by about 30 min. This experiment explored the dependence of Etomid and B_ (8901) on mice and rats. Since the effective duration of Etanercept and B_ (8901) was less than 90 minutes in less than half of that of morphine, it was administered 4 times daily and morphine was administered twice a day. In mice, using a jump test, the result is: equivalent analgesic dose escalation