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选择性κ-阿片受体激动剂U-50,488H对大鼠吗啡依赖的影响。

Effects of a selective kappa-opioid agonist, U-50,488H, on morphine dependence in rats.

作者信息

Fukagawa Y, Katz J L, Suzuki T

机构信息

Department of Pharmacology, Hoshi University, Japan.

出版信息

Eur J Pharmacol. 1989 Oct 24;170(1-2):47-51. doi: 10.1016/0014-2999(89)90132-5.

DOI:10.1016/0014-2999(89)90132-5
PMID:2558895
Abstract

Rats were made dependent on morphine by mixing the drug with their only source of food. Naltrexone (0.5 mg/kg) injection precipitated a syndrome of withdrawal signs including weight loss. Pretreatment with the selective kappa agonist, U-50,488H (1.0, 30.0 or 10.0 mg/kg), generally had no effects on the signs of morphine withdrawal. In other subjects, U-50,488H was repeatedly administered (1.0, 3.0 or 10.0 mg/kg per 12 h) during the development of morphine dependence. In these subjects, the course of naltrexone-precipitated withdrawal was unchanged. These results suggest that agonist activity at kappa receptors is not sufficient to alter morphine dependence or withdrawal.

摘要

通过将吗啡与大鼠唯一的食物来源混合,使大鼠对吗啡产生依赖。注射纳曲酮(0.5毫克/千克)引发了包括体重减轻在内的戒断症状综合征。用选择性κ阿片受体激动剂U-50,488H(1.0、30.0或10.0毫克/千克)进行预处理,通常对吗啡戒断症状没有影响。在其他实验对象中,在吗啡依赖形成过程中反复给予U-50,488H(每12小时1.0、3.0或10.0毫克/千克)。在这些实验对象中,纳曲酮引发的戒断过程没有改变。这些结果表明,κ阿片受体的激动剂活性不足以改变吗啡依赖或戒断。

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1
Effects of a selective kappa-opioid agonist, U-50,488H, on morphine dependence in rats.选择性κ-阿片受体激动剂U-50,488H对大鼠吗啡依赖的影响。
Eur J Pharmacol. 1989 Oct 24;170(1-2):47-51. doi: 10.1016/0014-2999(89)90132-5.
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The kappa-opioid receptor agonist U50,488H induces acute physical dependence in guinea-pigs.κ-阿片受体激动剂U50,488H可诱导豚鼠产生急性身体依赖性。
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A selective kappa-opioid agonist, U-50,488H, blocks the development of tolerance to morphine analgesia in rats.
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Effects of nor-binaltorphimine on the development of analgesic tolerance to and physical dependence on morphine.去甲纳曲酮对吗啡镇痛耐受性及身体依赖性形成的影响。
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Effects of morphine in rats treated chronically with U-50,488 H, a kappa opioid receptor agonist.κ阿片受体激动剂U-50,488 H长期处理的大鼠中吗啡的作用
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Withdrawal contractures of guinea-pig isolated ileum after acute activation of kappa-opioid receptors.κ-阿片受体急性激活后豚鼠离体回肠的戒断挛缩
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The selective kappa-opioid agonist, U-50,488H, produces antinociception in the rat via a supraspinal action.选择性κ阿片受体激动剂U-50,488H通过脊髓上作用在大鼠中产生抗伤害感受。
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