摘要
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。
An analgesic effect of PD134308 was studied in mice using a 50℃warm water tail - withdrawal assay. PD134308 produced analgesia dose - dependently(10 - 320 mg· kg -1). The analgesia induced by PD134308 was antagonized by naltrexone, but potentiated by SCH 32615, an enkephalinase inhibitor. The analgesic effect ofmorphine was enhanced by PD 134308, but attenuated by CCK - 4. However, PD 134308had no ettect on the clonidine - induced analgesia. These data suggest that PD 134308induced analgesia could be produced through an augmentation of endogenous opioids.
