Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
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发表时间：
1994-02
影响因子：
3.6
通讯作者：
K. Raynor;Hayeoung Kong;Yan Chen;K. Yasuda;Lei Yu;G. Bell;T. Reisine
中科院分区：
文献类型：
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作者：
K. Raynor;Hayeoung Kong;Yan Chen;K. Yasuda;Lei Yu;G. Bell;T. Reisine
阿片类药物，如吗啡和内源性阿片肽，即脑啡肽、内啡肽和强啡肽，发挥广泛的生理和行为作用，包括对疼痛感知、情绪、运动控制和自主功能的影响。这些作用是通过膜结合受体介导的，其中最具特征的是 kappa、delta 和 mu 受体。最近通过分子克隆证实了这些不同类型的阿片受体的存在。在本研究中，我们使用一系列广泛使用的阿片类药物检查了克隆的 kappa、delta 和 mu 受体的药理学特征。我们的结果表明，克隆的 kappa 和 mu 受体分别具有与内源表达的 kappa 1 和 mu 受体相似的药理学特征。克隆的δ受体表现出与δ2受体一致的药理学特征。具有滥用潜力的阿片类药物对 mu 受体具有高亲和力。克隆受体的可用性将有助于鉴定和开发更具特异性和选择性的化合物，这些化合物具有更大的治疗潜力和更少的不良副作用。
Opioid drugs, such as morphine, and the endogenous opioid peptides, namely the enkephalins, endorphins, and dynorphins, exert a wide spectrum of physiological and behavioral effects, including effects on pain perception, mood, motor control, and autonomic functions. These effects are mediated via membrane-bound receptors, of which the best characterized are the kappa, delta, and mu receptors. The existence of these distinct types of opioid receptors has recently been confirmed by molecular cloning. In the present study, we have examined the pharmacological profiles of the cloned kappa, delta, and mu receptors using a battery of widely employed opioid agents. Our results suggest that the cloned kappa and mu receptors have pharmacological characteristics similar to those of the endogenously expressed kappa 1 and mu receptors, respectively. The cloned delta receptor displays a pharmacological profile consistent with that of a delta 2 receptor. Opioid agents with abuse potential possess high affinities for the mu receptor. The availability of the cloned receptors will facilitate the identification and development of more specific and selective compounds with greater therapeutic potential and fewer undesirable side effects.