不同阿片受体在羟考酮引起小鼠高活动性和镇痛过程中的作用

Effects of different kinds of opiate receptor on oxycodone-induced hyperlococomotor and analgesia in mice

目的研究μ、δ、κ三种阿片受体在羟考酮引起小鼠高活动性和镇痛过程中的作用。方法采用小动物自主活动测定和热板镇痛实验方法。结果羟考酮(1.25,2.5,5.0mg.kg-1,s.c)使小鼠的自发活动明显增加,并成明显的量效关系。非选择性阿片受体拮抗剂naloxone能剂量依赖性的降低羟考酮引起的小鼠自发活动增加。选择性μ受体拮抗剂naloxonazine对羟考酮(5.0mg.kg-1,s.c)引起的小鼠自发活动增加没有影响,而选择性δ受体拮抗剂naltrindole能剂量依赖性的降低羟考酮引起的小鼠自发活动的增加,选择性κ受体拮抗剂nor-Binltorphimine增强羟考酮引起小鼠高活动性的作用;naloxonazine和naltrindol不影响羟考酮的镇痛作用,而nor-Binltorphimine能拮抗羟考酮的镇痛作用。结论羟考酮引起小鼠自发活动增加可能是通过δ介导的,而羟考酮的镇痛作用可能是通过κ受体介导的。

Aim To investage the effects of μ、δ、κ-receptor on hyperlocomotor and analgesia in mice.Methods Locomotor activity experiment and hot-plate pain experiment were measured.Results Oxycodone dose-dependently enhanced locomotor response in mice.Naloxone,a unselective opioid receptor antagonists and naltrindole（δ-selective opioid receptor antagonist）could attenuate the increase of locomotor acitivity induced by oxycodone,but naloxonazine,a μ-receptor antagonist had no such effect.κ-receptor antagonist nor-Binltorphimine increased hyperlocomotion induced by oxycodone.In antinociceptive experiment,naloxonazine and naltrindole could not attenuate the that of oxycodone,but nor-Binaltorphimine could attenuate the antinociceptive effects of oxycodone.Conclusion Oxycodone-hyperlocomotor is probably mediated by δ opioid receptor,and antinocieptive effects of oxycodone is probably mediated by κ opioid receptor.