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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >κ-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system
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κ-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system

机译：人的κ阿片受体：cDNA和基因组克隆，染色体分配，功能表达，药理学和中枢神经系统中的表达方式

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摘要

Using the mouse δ-opioid receptor cDNA as a probe, we have isolated genomic clones encoding the human μ- and κ-opioid receptor genes. Their organization appears similar to that of the human δ receptor gene, with exon-intron boundaries located after putative transmembrane domains 1 and 4. The κ gene was mapped at position q11-12 in human chromosome 8. A full-length cDNA encoding the human κ-opioid receptor has been isolated. The cloned receptor expressed in COS cells presents a typical κ1 pharmacological profile and is negatively coupled to adenylate cyclase. The expression of κ-opioid receptor mRNA in human brain, as estimated by reverse transcription-polymerase chain reaction, is consistent with the involvement of κ-opioid receptors in pain perception, neuroendocrine physiology, affective behavior, and cognition. In situ hybridization studies performed on human fetal spinal cord demonstrate the presence of the transcript specifically in lamina Ⅱ of the dorsal horn. Some divergences in structural, pharmacological, and anatomical properties are noted between the cloned human and rodent receptors.
机译：使用小鼠δ阿片受体cDNA作为探针，我们分离出了编码人μ和κ阿片受体基因的基因组克隆。它们的组织看起来与人δ受体基因的组织相似，外显子-内含子边界位于推定的跨膜结构域1和4之后。κ基因定位在人染色体8的q11-12位置。编码人的全长cDNA κ阿片受体已经分离。在COS细胞中表达的克隆受体具有典型的κ1药理作用，并且与腺苷酸环化酶呈负相关。通过逆转录-聚合酶链反应估计，人脑中κ阿片受体mRNA的表达与κ阿片受体在疼痛感知，神经内分泌生理，情感行为和认知中的参与一致。在人类胎儿脊髓上进行的原位杂交研究表明，该转录本特别存在于背角Ⅱ层。在克隆的人类和啮齿动物受体之间在结构，药理和解剖学特性上存在一些差异。

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