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用小鼠热水缩尾法研究了高选择性的CCK-B受体拮抗剂PD134308的镇痛效应。PD134308在小鼠产生的镇痛有剂量依赖关系。阿片受体拮抗剂对抗其镇痛作用,表明阿片受体系统参与介导PD134308的镇痛。PD134308能加强吗啡的镇痛作用,但对α2受体激动剂可乐定的镇痛作用没有影响,表明CCK-B受体拮抗剂对阿片受体系统作用有选择性。脑啡肽酶抑制剂SCH32615加强PD134308的镇痛作用,说明PD134308可能是通过增加内源性阿片物质产生镇痛作用的。另外,PD134308还参与吗啡镇痛耐受性的形成。
The analgesic effect of the highly selective CCK-B receptor antagonist PD134308 was investigated using mouse hot-water tailing. PD134308 produced a dose-dependent analgesia in mice. Opioid receptor antagonists counteract their analgesic effects, indicating that the opioid receptor system is involved in mediating the analgesia of PD134308. PD134308 enhanced the analgesic effect of morphine but had no effect on the analgesic effect of clonidine, an alpha 2 receptor agonist, suggesting that CCK-B receptor antagonists have a selective effect on the opioid receptor system. Enkephalinase inhibitor SCH32615 enhances the analgesic effect of PD134308, indicating that PD134308 may have an analgesic effect by increasing endogenous opioid. In addition, PD134308 is also involved in the development of morphine analgesia tolerance.