目的研究戒毒康对吗啡依赖豚鼠离体回肠催促戒断反应的抑制作用。方法连续递增皮下注射吗啡,建立豚鼠身体依赖性模型,利用MD2000 Super Lab生物信息采集系统观察戒毒康对纳洛酮催促诱发吗啡身体依赖性豚鼠离体回肠的戒断性收缩的抑制作...目的研究戒毒康对吗啡依赖豚鼠离体回肠催促戒断反应的抑制作用。方法连续递增皮下注射吗啡,建立豚鼠身体依赖性模型,利用MD2000 Super Lab生物信息采集系统观察戒毒康对纳洛酮催促诱发吗啡身体依赖性豚鼠离体回肠的戒断性收缩的抑制作用。结果戒毒康高(0.6 mg.mL-1)、中(0.3 mg.mL-1)、低(0.15 mg.mL-1)3个剂量对吗啡依赖豚鼠离体回肠纳洛酮催促戒断性收缩的抑制率分别为:78.8%,46.8%,30.0%,并呈剂量相关性,其中高剂量组和中剂量组与模型组比较,有显著性差异。结论戒毒康在一定程度上能抑制吗啡依赖豚鼠离体回肠体外纳洛酮催促戒断性收缩。展开更多
AIM: To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro . METHODS: The effects of thienorphine on intestinal transit were examined in mice and...AIM: To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro . METHODS: The effects of thienorphine on intestinal transit were examined in mice and in isolated GPI. Buprenorphine and morphine served as controls. The distance traveled by the head of the charchol and the total length of the intestine were measured in vivo . Gastrointestinal transit was expressed as a percentage of the distance traveled by the head of the marker relative to the total length of the small intestine. The isolated GPI preparations were connected to an isotonic force transducer and equilibrated for at least 1 h before exposure to drugs. Acetylcholine was used for muscle stimulation. RESULTS: Thienorphine (0.005-1.0 mg/kg, ig ) or bu-prenorphine (0.005-1.0 mg/kg, sc ) dose-dependently significantly inhibited gut transit compared with saline. Thienorphine inhibited gut transit less than buprenorphine. The maximum inhibition by thienorphine on the intestinal transit was 50%-60%, whereas the maximum inhibition by morphine on gut transit was about 100%. Thienorphine also exhibited less inhibition on acetylcholine-induced contraction of GPI, with a maximum inhibition of 65%, compared with 93% inhibition by buprenorphine and 100% inhibition by morphine. Thienorphine induced a concentration-dependent decrease in the basal tonus of spontaneous movement of the GPI, the effect of which was weaker than that with buprenorphine. The duration of the effect of thienorphine on the GPI was longer than that with buprenorphine. CONCLUSION: Thienorphine had less influence, but a longer duration of action on GPI contraction and moderately inhibited intestinal transit.展开更多
基金Supported by National New Drugs Foundation of China, No.2011ZX09101-005-01"Integrated Drug Discovery Technology Plat form" of National Science and Technology Major Projects for "Major New Drugs Innovation and Development", No.2012ZX09301003-001
文摘AIM: To evaluate the effect of thienorphine on small intestinal transit in vivo and on guinea-pig ileum (GPI) contraction in vitro . METHODS: The effects of thienorphine on intestinal transit were examined in mice and in isolated GPI. Buprenorphine and morphine served as controls. The distance traveled by the head of the charchol and the total length of the intestine were measured in vivo . Gastrointestinal transit was expressed as a percentage of the distance traveled by the head of the marker relative to the total length of the small intestine. The isolated GPI preparations were connected to an isotonic force transducer and equilibrated for at least 1 h before exposure to drugs. Acetylcholine was used for muscle stimulation. RESULTS: Thienorphine (0.005-1.0 mg/kg, ig ) or bu-prenorphine (0.005-1.0 mg/kg, sc ) dose-dependently significantly inhibited gut transit compared with saline. Thienorphine inhibited gut transit less than buprenorphine. The maximum inhibition by thienorphine on the intestinal transit was 50%-60%, whereas the maximum inhibition by morphine on gut transit was about 100%. Thienorphine also exhibited less inhibition on acetylcholine-induced contraction of GPI, with a maximum inhibition of 65%, compared with 93% inhibition by buprenorphine and 100% inhibition by morphine. Thienorphine induced a concentration-dependent decrease in the basal tonus of spontaneous movement of the GPI, the effect of which was weaker than that with buprenorphine. The duration of the effect of thienorphine on the GPI was longer than that with buprenorphine. CONCLUSION: Thienorphine had less influence, but a longer duration of action on GPI contraction and moderately inhibited intestinal transit.
