Primary structure and functional expression of a guinea pig kappa opioid (dynorphin) receptor.
Primary structure and functional expression of a guinea pig kappa opioid (dynorphin) receptor.
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豚鼠卡帕阿片（强啡肽）受体的一级结构和功能表达。
DOI：
10.1073/pnas.91.9.3779
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发表时间：
1994
影响因子：
11.1
通讯作者：
Akil,H
中科院分区：
文献类型：
--
作者：
Xie,GX;Meng,F;Mansour,A;Thompson,RC;Hoversten,MT;Goldstein,A;Watson,SJ;Akil,H
编码豚鼠 kappa 阿片样物质（强啡肽）受体的全长 cDNA 已被分离出来。推导的蛋白质包含 380 个氨基酸和 7 个 G 蛋白偶联受体特征的疏水性 α 螺旋。该受体与小鼠和大鼠的 kappa 受体有 90% 相同，其中 N 末端区域的差异最大。当在 COS-7 细胞中表达时，该受体对强啡肽和其他 kappa 选择性阿片类配体（例如 U50、488）表现出高亲和力和立体特异性。它不结合 mu 和 delta 选择性阿片类配体。表达的受体与 G 蛋白功能性偶联，抑制腺苷酸环化酶和 Ca2+ 通道。豚鼠 kappa 受体 mRNA 在许多大脑区域表达，包括小脑，这种模式与经典豚鼠 kappa 结合位点的放射自显影图非常吻合。克隆豚鼠和大鼠 kappa 受体之间药理学和 mRNA 分布的物种差异可能值得进一步研究。
A full-length cDNA encoding the guinea pig kappa opioid (dynorphin) receptor has been isolated. The deduced protein contains 380 aa and seven hydrophobic alpha-helices characteristic of the G protein-coupled receptors. This receptor is 90% identical to the mouse and rat kappa receptors, with the greatest level of divergence in the N-terminal region. When expressed in COS-7 cells, the receptor displays high affinity and stereospecificity toward dynorphin peptides and other kappa-selective opioid ligands such as U50, 488. It does not bind the mu- and delta-selective opioid ligands. The expressed receptor is functionally coupled to G protein(s) to inhibit adenylyl cyclase and Ca2+ channels. The guinea pig kappa receptor mRNA is expressed in many brain areas, including the cerebellum, a pattern that agrees well with autoradiographic maps of classical guinea pig kappa binding sites. Species differences in the pharmacology and mRNA distribution between the cloned guinea pig and rat kappa receptors may be worthy of further examination.