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首页> 外文期刊>BMC Neuroscience >Delta-opioid receptor endocytosis in spinal cord after dermenkephalin activation
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Delta-opioid receptor endocytosis in spinal cord after dermenkephalin activation

机译：脑啡肽激活后脊髓中的δ阿片受体内吞作用

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Background The delta(δ)-opioid receptors belong to the G protein-coupled receptors and in vitro studies have shown that δ-opioid receptors undergo an internalization process in response to agonist stimulation. The immediate consequence is the disappearance of receptors from the plasma membrane. This adaptation process reveals the cell's capacity to desensitize after a strong agonist stimulus. This process, if it occurs in vivo , could contribute to the tolerance phenomenon observed after opiate treatment. To study the mechanisms underlying regulation of the δ-opioid receptors in vivo , the effects of an application of the drug dermenkephalin, a potent and selective agonist of the δ-opioid receptor, were analysed in the rat spinal cord. Results Using immunocytochemistry and electron microscopy, we observed in control rats that membrane labelling was strictly localized at the interface between two neurites. Fifteen minutes after dermenkephalin stimulation, the plasma membrane labelling was associated with invaginated areas. Thirty minutes after stimulation, labelled vesicles were found in the cytoplasm confirming the internalization process. Conclusions The present findings support the view that δ-opioid receptors are internalized in response to prolonged exposure to dermenkephalin in vivo and confirm the presynaptic localization of δ-opioid receptors in the dorsal horn of the rat spinal cord.
机译：背景技术δ（δ）-阿片样物质受体属于G蛋白偶联受体，并且体外研究表明δ-阿片样物质受体响应激动剂刺激而经历内在化过程。直接后果是质膜中受体的消失。这种适应过程揭示了细胞在强烈的激动剂刺激后脱敏的能力。如果此过程在体内发生，则可能有助于鸦片制剂治疗后观察到的耐受现象。为了研究体内调节δ-阿片样物质受体的潜在机制，在大鼠脊髓中分析了药物δ-阿片受体的有效成分和选择性激动剂dermenkephalin的应用效果。结果使用免疫细胞化学和电子显微镜观察，我们在对照组大鼠中观察到膜标记严格位于两个神经突之间的界面。 dermenkephalin刺激后十五分钟，质膜标记与内陷区域相关。刺激后三十分钟，在细胞质中发现了标记的囊泡，证实了内在化过程。结论目前的发现支持这样的观点，即δ-阿片受体在体内长期暴露于苯甲脑啡素中被内化，并证实了δ-阿片受体在大鼠脊髓背角中的突触前定位。

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