脑室注射ACTH对抗羟甲芬太尼引起的镇痛  

Antagonism of ohmefentanyl analgesia by intraceretroventriculal injection of adrenocortitropic hormone in rats

作　　者：李显喜 方园[1] 韩济生[1] 

机构地区：[1]北京医科大学生理学系,卫生部脑功能研究重点实验室,北京医科大学生物化学与分子生物学系

出　　处：《中国药理学通报》1996年第3期221-223,共3页Chinese Pharmacological Bulletin

摘　　要：通常中枢注射促肾上腺皮质激素（ＡＣＴＨ）能够拮抗阿片的镇痛作用，然而其机制尚未阐明。本实验用辐射热─甩尾法测定痛阈，ｓｃｍｕ型阿片受体高选择性激动剂──羟甲芬太尼（０．８μｇ·ｋｇ－１），引起明显的镇痛效应，然后ｉｃｖＡＣＴＨ。发现小剂量的ＡＣＴＨ（１５．６～２５０ｎｇ）即可剂量依赖性抑制羟甲芬太尼的镇痛效应，其最大抑制率为７７．３％，半数有效量为１０７ｎｇ。单独注射ＡＣＴＨ２５０ｎｇ对基础病阈无影响。结果提示，ＡＣＴＨ在ｍｕ型阿片受体介导的镇痛中起重要作用。The effects of adrenocortitropic hormone(ACTH)on opiate-induced analgesia have been investigated for many years.When centrally administered,ACTH usually prevent the analgesia action of opiate though the mechanism of the blockade was obscure.In the present study,we used the potent mu-opiate receptor agonist ohmefentanyl(OMF)to produce analgesis,then treated With ACTH1～24 by intraceretroventriculal injection(icv). Effects on nociceptive thresholds using the tail flick test were observed.We found that small doses of ACTH(15.6～250 ng)could dose-dependently eliminate the analgesia effect caused by OMF(sc 0.8 μg·kg-1).The maximal inhibition rate was 77.3% and the ED50 was 107 ng.ACTH1～24(250 ng,icv)showed no significant effect on the basal nociceptive state of rats.The results suggested ACTH1～ 24 may Play an important role in mu-opiate recegtor mediated analgesia.

关 键 词：羧甲芬太尼 mu型阿片受体 镇痛 ACTH 

分 类 号：R977.11[医药卫生—药品]