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μ-阿片受体基因敲除小鼠中无海洛因或吗啡6β-葡萄糖醛酸苷镇痛作用。

No heroin or morphine 6beta-glucuronide analgesia in mu-opioid receptor knockout mice.

作者信息

Kitanaka N, Sora I, Kinsey S, Zeng Z, Uhl G R

机构信息

Molecular Neurobiology Branch, National Institute on Drug Abuse, Intramural Research Program, Baltimore, MD 21224, USA.

出版信息

Eur J Pharmacol. 1998 Aug 14;355(1):R1-3. doi: 10.1016/s0014-2999(98)00516-0.

DOI:10.1016/s0014-2999(98)00516-0
PMID:9754945
Abstract

Recent reports suggest that heroin and its metabolite morphine 6beta-glucuronide can produce analgesia independent of the morphine-preferring mu-opioid receptor. We have tested heroin and morphine 6beta-glucuronide analgesia in wild-type, homozygous and heterozygous mu-opioid receptor knockout mice. Homozygotes display no heroin or morphine 6beta-glucuronide analgesia. Heterozygous mice with one mu-opioid receptor gene copy reveal reduced heroin and morphine 6beta-glucuronide analgesia. The mu-opioid receptor-dependence of heroin and morphine 6beta-glucuronide fails to support a requirement for a heroin-specific opiate receptor subtype.

摘要

最近的报告表明,海洛因及其代谢产物吗啡6β-葡萄糖醛酸苷可产生不依赖于吗啡偏好性μ-阿片受体的镇痛作用。我们在野生型、纯合子和杂合子μ-阿片受体基因敲除小鼠中测试了海洛因和吗啡6β-葡萄糖醛酸苷的镇痛作用。纯合子未表现出海洛因或吗啡6β-葡萄糖醛酸苷的镇痛作用。具有一个μ-阿片受体基因拷贝的杂合子小鼠显示出海洛因和吗啡6β-葡萄糖醛酸苷的镇痛作用减弱。海洛因和吗啡6β-葡萄糖醛酸苷对μ-阿片受体的依赖性不支持存在海洛因特异性阿片受体亚型的需求。

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