摘要
目的探讨5-羟色胺(5-hydroxytryptamine,5-HT)2A受体拮抗剂MDL11939在急性乙酸内脏痛、急性切口痛和坐骨神经慢性缩窄性损伤(chronic constrictive injury,CCI)模型中发挥的作用及意义。方法选用♂昆明小鼠,建立急性乙酸内脏痛、急性切口痛和CCI神经病理性痛模型,通过腹腔注射给药,观察乙酸致小鼠扭体反应次数变化、切口痛和CCI痛患侧热缩足反射潜伏期(thermal withdrawal latency,TWL)变化。结果在小鼠急性乙酸内脏痛模型中,与溶剂对照组相比,MDL11939(0.25、0.5、1.0 mg·kg^(-1),i.p.)呈剂量依赖性地减轻乙酸内脏痛,扭体反应次数明显减少。在急性切口痛和CCI模型中,与模型组和自身给药前相比,MDL11939(0.5 mg·kg^(-1),i.p.)可以明显提高小鼠患侧的热缩足阈值,减轻疼痛。结论 MDL11939通过腹腔系统性给药可以有效地减轻急性乙酸内脏痛、急性切口痛和CCI慢性神经病理性痛。
Aim To investigate the effects and signifi-cance of 5-HT2A receptor antagonist MDL1 1 939 on a-mice.Methods Kunming male mice were suffered a-cute acetic acid visceral pain,acute incision pain and CCI neuropathic pain.After each animal model was es-tablished,MDL1 1 939 was injected intraperitoneally. The writhing reaction was used to assess acute acetic acid visceral pain,while the thermal withdrawal laten-cy （TWL）was used to evaluate the acute incision pain and CCI neuropathic pain.Results Compared with the control group,MDL1 1 939 （0.25,0.5,1 .0 mg·kg^ -1 ,i.p.）relieved acetic acid visceral pain signifi-cantly in a dose-dependent manner in mice,as re-vealed by the significant reduction of the number of twisting.In acute incision pain and CCI neuropathic pain,MDL1 1 939 （0.5 mg·kg^-1 ,i.p.）significantly increased TWL level.Conclusion 5-HT2A receptor antagonist MDL1 1 939 has analgesic effects on visceral pain,acute pain and neuropathic pain,which might be a novel therapeutic target to treat different pain in clini-cal situations.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2017年第2期223-227,共5页
Chinese Pharmacological Bulletin
基金
国家自然科学基金资助项目(No81171041,81271217)
江苏省高校自然科学基金重点项目(No13KJA320001)
江苏省自然科学基金资助项目(NoBK20161171)
