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Non-opioid actions of opioid peptides.

机译：阿片肽的非阿片作用。

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Beside the well known actions of opioid peptides on mu-, delta- and kappa-opioid receptors, increasing amount of pharmacological and biochemical evidence has recently been published about non-opioid actions of various opioid peptides. These effects are not abolished by naloxone treatments. Such non-opioid effects are observed both in nervous tissues and in the cellular elements of the immune system. Peptides exhibiting non-opioid effects include beta-endorphin, dynorphin A, nociceptin/OFQ, endomorphins, hemorphins and a number of Proenkephalin A derived peptides, such as Met-enkephalin, Met-enkephalin-Arg-Phe (MERF) and bovine adrenal medullary peptide (BAM22). Non-opioid actions are exerted through different neuronal receptors, e.g., dynorphin hyperalgesia through NMDA receptor, Met-enkephalin induced regulation of cell growth through zeta receptors, pain modulation by nociceptin through ORL-1 or NOP receptors, while BAM22 acts through sensory neuron specific G protein-coupled receptors (SNSR). We have investigated Met-enkephalin-Arg-Phe (MERF) and its analogues by the means of direct and indirect radioligand binding assays. It has been found that in addition to kappa(2) and delta-opioid receptors, MERF can act also through sigma(2)- or probably via FMRF-NH(2) receptors in rat cerebellum. A role of functionally assembling heterodimer receptors in mediating the non-conventional actions of these peptide ligands can not be excluded as well.
机译：除了已知的阿片肽对μ-，δ-和阿片受体的作用外，最近还公开了越来越多的有关各种阿片肽的非阿片作用的药理和生化证据。纳洛酮治疗不能消除这些作用。在神经组织和免疫系统的细胞成分中均观察到这种非阿片样物质的作用。表现出非阿片样物质作用的肽包括β-内啡肽，强啡肽A，伤害感受肽/ OFQ，内啡肽，血红素和许多前脑啡肽A衍生的肽，例如Met-脑啡肽，Met-脑啡肽-Arg-Phe（MERF）和牛肾上腺髓质肽（BAM22）。非阿片类药物的作用通过不同的神经元受体发挥作用，例如通过NMDA受体引起强啡肽痛觉过敏，Met-脑啡肽通过zeta受体诱导细胞生长调节，痛觉肽通过ORL-1或NOP受体调节疼痛，而BAM22通过感觉神经元特异性作用G蛋白偶联受体（SNSR）。我们已经通过直接和间接放射性配体结合测定法研究了Met-脑啡肽-Arg-Phe（MERF）及其类似物。已经发现，除了kappa（2）和δ阿片样物质受体外，MERF还可以通过sigma（2）-或可能通过大鼠小脑中的FMRF-NH（2）受体起作用。也不能排除功能性组装异二聚体受体在介导这些肽配体的非常规作用中的作用。

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