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首页> 外文期刊>BMC Neuroscience >Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors
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Activation profiles of opioid ligands in HEK cells expressing δ opioid receptors

机译：表达δ阿片受体的HEK细胞中阿片配体的活化特性。

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Background The aim of the present study was to characterize the activation profiles of 15 opioid ligands in transfected human embryonic kidney cells expressing only δ opioid receptors. Activation profiles of most of these ligands at δ opioid receptors had not been previously characterized in vitro . Receptor activation was assessed by measuring the inhibition of forskolin-stimulated cAMP production. Results Naltrexone and nalorphine were classified as antagonists at δ opioid receptor. The other ligands studied were agonists at δ opioid receptors and demonstrated IC50 values of 0.1 nM to 2 μM, maximal inhibition of 39–77% and receptor binding affinities of 0.5 to 243 nM. The rank order of efficacy of the ligands tested was metazocine = xorphanol ≥ fentanyl = SKF 10047 = etorphine = hydromorphone = butorphanol = lofentanil > WIN 44,441 = Nalbuphine = cyclazocine ≥ met-enkephalin morphine = dezocine. For the first time these data describe and compare the function and relative efficacy of several ligands at δ opioid receptors. Conclusions The data produced from this study can lead to elucidation of the complete activation profiles of several opioid ligands, leading to clarification of the mechanisms involved in physiological effects of these ligands at δ opioid receptors. Furthermore, these data can be used as a basis for novel use of existing opioid ligands based on their pharmacology at δ opioid receptors.
机译：背景技术本研究的目的是表征仅表达δ阿片受体的转染人胚胎肾细胞中15种阿片配体的活化特性。这些配体在δ阿片受体上的活化谱以前尚未在体外鉴定。通过测量对福斯高林刺激的cAMP产生的抑制来评估受体的活化。结果纳曲酮和纳洛啡被认为是δ阿片受体的拮抗剂。研究的其他配体是δ阿片受体的激动剂，并证明IC 50 值为0.1 nM至2μM，最大抑制率为39–77％，受体结合亲和力为0.5至243 nM。所测试配体的功效等级为：间佐辛= xorphanol≥芬太尼= SKF 10047 =依托芬=氢吗啡酮=丁啡烷=洛芬太尼> WIN 44,441 =萘丁碱=环唑烷≥甲脑啡吗啡=地佐辛。这些数据首次描述并比较了δ阿片受体上几种配体的功能和相对功效。结论从这项研究中获得的数据可以阐明几种阿片样物质配体的完整活化特性，从而阐明这些配体对δ阿片受体的生理作用所涉及的机制。此外，基于它们在δ阿片受体上的药理作用，这些数据可以用作现有阿片配体新用途的基础。

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