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Mechanism of action of anti-opioid peptides at pain syndrome

机译:抗阿片类肽在疼痛综合征中的作用机制

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An important goal of modern medicinal chemistry is to study the mechanisms of pain and analgesia in order to design effective analgesic drugs. Opioid analgesics are the gold standard for the treatment of severe pain; however, the use of opiates is associated with the development of side effects which are, in particular, related to the activation of the anti-opioid system. Mammalians synthesize a number of endogenous peptides, such as orphanin FGGFTGARKSARKLANQ, neuropeptide FF (FLFQPQRF-NH2), tripeptide melanostatin (MIF) PLG-NH2, as well as related compounds. These anti-opioid peptides are to one extent or another involved in homeostatic control of transmission of pain impulses. The present review includes the data published to date in domestic and foreign literature on the involvement of these peptides in such undesirable phenomena as inhibition of opioid analgesia, development of opioid tolerance and dependence, and hyperalgesia. Cell-cell and molecular ligand-receptor and receptor-receptor interactions of the opioid and anti-opioid systems are considered. These data can be useful for the design of new pharmaceuticals for pain relief. The generalization and study of these mechanisms are reflected in various approaches to treatment of pain syndromes and require analysis and further investigation.
机译:现代医药化学的一个重要目标是研究疼痛和镇痛的机制,以设计有效的镇痛药。阿片类镇痛药是治疗严重疼痛的金标准;然而,使用蛋白质的使用与副作用的发展有关,特别是与抗阿片类药物的活化有关。哺乳动物合成许多内源性肽,例如孤儿林FGGFRGARKSARKLANQ,神经肽FF(FLFQPQRF-NH2),三肽素抑制菌素(MIF)PLG-NH2,以及相关的化合物。这些抗阿片类肽在一定程度上或另一个涉及患有疼痛脉冲传播的稳态控制。本综述包括在国内外文学中发布的数据,这些数据与这些肽在这种不良现象中的抑制作用,作为阿片类镇痛的抑制,表述耐受性和依赖性和痛觉过敏。考虑细胞 - 细胞和分子配体 - 受体和阿片类药物和抗阿片类药物的受体相互作用。这些数据对于设计新药物的疼痛缓解是有用的。这些机制的泛化和研究反映在各种方法中,治疗疼痛综合征,需要进行分析和进一步调查。

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