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阿片受体在急性和慢性给予阿片类药物增强戊巴比妥睡眠时间方面的作用。

The role of opiate receptors in the potentiation of pentobarbital sleeping time by the acute and chronic administration of opiates.

作者信息

Pechnick R N, Terman G W

机构信息

Department of Pharmacology, School of Medicine, U.C.L.A. 90024.

出版信息

Neuropharmacology. 1987 Nov;26(11):1589-93. doi: 10.1016/0028-3908(87)90006-2.

Abstract

Male rats injected with pentobarbital (50.0 mg/kg i.p.) showed increased sleeping time after the acute administration of morphine (5.0 or 10.0 mg/kg s.c.). This effect was antagonized by naltrexone (2.0 mg/kg s.c.). The enhancement displayed stereoselectivity as levorphanol greatly lengthened the sleeping time induced by pentobarbital while dextrophan only produced a slight increase. Rats implanted for 3 days with pellets of morphine base (75.0 mg) were tolerant to the analgesic effects of morphine (2.5 mg/kg s.c.) but showed an even greater increase in pentobarbital-induced sleeping time than rats treated acutely. No potentiation was observed in subjects that were also implanted with a pellet of naltrexone (30.0 mg). It is concluded that the potentiation of pentobarbital-induced sleeping time produced by opiates is mediated by opiate receptors, but fails to show the development of tolerance.

摘要

腹腔注射戊巴比妥(50.0毫克/千克)的雄性大鼠,在皮下注射吗啡(5.0或10.0毫克/千克)急性给药后睡眠时间增加。这种作用被纳曲酮(2.0毫克/千克皮下注射)拮抗。这种增强表现出立体选择性,因为左啡诺极大地延长了戊巴比妥诱导的睡眠时间,而右啡烷仅产生轻微增加。植入吗啡碱丸(75.0毫克)3天的大鼠对吗啡(2.5毫克/千克皮下注射)的镇痛作用产生耐受,但与急性处理的大鼠相比,戊巴比妥诱导的睡眠时间增加甚至更大。在同时植入纳曲酮丸(30.0毫克)的实验对象中未观察到增强作用。得出的结论是,阿片类药物对戊巴比妥诱导的睡眠时间的增强作用是由阿片受体介导的,但未表现出耐受性的发展。

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