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μ阿片受体:cDNA克隆与表达

mu opiate receptor: cDNA cloning and expression.

作者信息

Wang J B, Imai Y, Eppler C M, Gregor P, Spivak C E, Uhl G R

机构信息

Molecular Neurobiology Branch, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD.

出版信息

Proc Natl Acad Sci U S A. 1993 Nov 1;90(21):10230-4. doi: 10.1073/pnas.90.21.10230.

Abstract

mu opiate receptors recognize morphine with high affinity. A 2.1-kb rat brain cDNA whose predicted translation product displays 63% identity with recently described delta and kappa opiate receptor sequences was identified through polymerase chain reaction and cDNA homology approaches. This cDNA recognizes a 10.5-kb mRNA that is expressed in thalamic neurons. COS-cell expression confers naloxonazine-, Na(+)-, and GTP-sensitive binding of mu but not delta or kappa opioid ligands. Expressing cells bind morphine, [D-Ala2,N-methyl-Phe4,glyol5]enkephalin (DAMGO), and [D-Ala2,D-Leu5]enkephalin (DADLE) with nanomolar or subnanomolar affinities, defining a mu opiate receptor that avidly recognizes analgesic and euphoric opiate drugs and opioid peptides.

摘要

μ阿片受体以高亲和力识别吗啡。通过聚合酶链反应和cDNA同源性方法,鉴定出一个2.1 kb的大鼠脑cDNA,其预测的翻译产物与最近描述的δ和κ阿片受体序列具有63%的同一性。该cDNA识别在丘脑神经元中表达的10.5 kb mRNA。COS细胞表达赋予μ阿片受体对纳洛嗪、Na⁺和GTP敏感的结合特性,但对δ或κ阿片样物质配体不敏感。表达细胞以纳摩尔或亚纳摩尔亲和力结合吗啡、[D - Ala²,N - 甲基 - Phe⁴,甘醇⁵]脑啡肽(DAMGO)和[D - Ala²,D - Leu⁵]脑啡肽(DADLE),定义了一种能 avidly识别镇痛和欣快阿片类药物及阿片肽的μ阿片受体。(注:avidly这个词在医学专业语境下不太好准确翻译,暂保留英文,可结合上下文进一步理解其准确含义)

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b82c/47748/8e056ba38f9e/pnas01528-0501-a.jpg

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