盐酸二氢埃托啡对小鼠、大鼠和豚鼠肠道平滑肌的作用

Effects of dihydroetorphine hydrochloride on intestinal smooth muscles in mice, rats and guinea pigs

目的：研究ＤＨＥ对肠道平滑肌的作用。方法：小鼠、大鼠和豚鼠离体和在体肠道平滑肌上，以吗啡为对照，比较ＤＨＥ与吗啡对肠道平滑肌作用的异同。结果：吗啡和ＤＨＥ减慢小鼠肠推进运动的ＥＤ５０分别为２．７９ｍｇ·ｋｇ－１和３．２３μｇ·ｋｇ－１；ＤＨＥ３６～６０μｇ·ｋｇ－１ｓｃ可松弛小鼠在体肠道平滑肌，在相同的实验条件下，吗啡５～２０ｍｇ·ｋｇ－１ｓｃ可剂量依赖性地收缩小鼠在体肠道平滑肌；在小鼠、大鼠和豚鼠离体肠管上，ＤＨＥ兴奋肠道平滑肌的浓度依次为１０～１００，０．１～１０和１０～１００μｍｏｌ·Ｌ－１，吗啡兴奋肠道平滑肌的浓度分别为０．１～１０，０．００２～２．０和０．１～１０μｍｏｌ·Ｌ－１，而ＤＨＥ兴奋肠道平滑肌的浓度是在镇痛剂量下体内无法达到的。结论：对肠道平滑肌作用，ＤＨＥ与吗啡不同，ＤＨＥ呈舒张效应，而吗啡为收缩效应。

AIM:To study the effects of dihydroetorphine hydrochloride(DHE) on intestinal smooth muscles. Methods: To evaluate the differences in the effects of DHE and morphine on the intestinal smooth muscles of mice, rats and guinea pigs. Results:The effects of DHE on intestinal smooth muscles derived from mice, rats and guinea pigs were studied in vivo and in vitro . In vivo experiments, DHE 36￣60 μg·kg -1 and morphine 5￣20 mg·kg -1 sc could dose dependently relax the mouse intestinal smooth muscles; the median effective doses of DHE and morphine for slowing the mouse intestinal peritalsis were 3 23 μg·kg -1 and 2 79 mg·kg -1 sc respectively. In the isolated intestine preparations derived from mice, rats and guinea pigs,the intestinal smooth muscles were contracted by DHE at the concentrations of 10￣100, 0 1￣10 0 and 10￣100 μmol·L -1 as well as by morphine at the concentrations of 0 1￣10,0 002￣2 0 and 0 1￣10 0 μmol·L -1 respectively. The excitatory effects on intestinal smooth muscles were induced by DHE at the concentrations much higher than its pharmacological effective doses for inducing analgesia. Conclusion: DHE produces the relaxation but morphine produces the contraction of intestinal smooth muscles.