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Effects of Peripherally Acting opioid Ligands on Central opioid Receptors and <i>β</i>-Endorphin Release in Stressed Rats

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Journal of Behavioral and Brain Science 2012年第2期2卷 162-166页

作者： Sergey K. Sudakov Valentina G. Bashkatova Tatiyana V. Proskuriakova Alexey E. Umriukhin P.K. Anokhin Research Institute of Normal Physiology RAMS Moscow Russia

Using the radioreceptor binding assay, μ-opioid receptor (MOR) affinity in the midbrain of stressed rats was higher than in naive controls. MOR density in the rat frontal cortex was reduced after stress. Intragastric administration of the MOR antagonist naloxone methiodide was followed by an increase in the number of MORs in the frontal cortex. However, the MOR agonist loperamide significantly decreased the density of MORs in the frontal cortex and midbrain of naive animals. Loperamide and naloxone methiodide were shown to prevent an increase in MOR affinity and a decrease in MOR density in the midbrain of rats after restraint stress. The restraint stress was accompanied by an increase in the release of β-endorphin (BE) in the ventral tegmental area (VTA) of control rats. After administration, loperamide slightly decreased the release of BE, naloxone methiodide significantly increased the release of BE in the cingulate cortex (CC) of untreated animals, while drugs had no effect on the release of BE in the VTA. The drugs significantly increased the extracellular level of BE in the CC of stressed animals. Loperamide abolished the increase in the stress-induced release of BE in the VTA. By contrast, naloxone methiodide significantly increased the release of BE in the VTA of stressed rats. Our data indicated that activation of peripheral MORs induces depression of the central part of the μ-opioid system, but suppression of peripheral MOR activity induces activation of the central μ-opioid system, the interaction of which can be modulated by stress.

关键词： Peripheral opioid Receptors Emotional Stress β-Endorphin Microdialysis Radioligand Binding Density of μ-opioid Receptors

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Effect of Mas-related gene（Mrg） receptors on hyperalgesia in rats with CFA-induced inflammation via direct and indirect mechanisms

Effect of Mas-related gene（Mrg） receptors on hyperalgesia ...

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中国神经科学学会第十届全国学术会议

作者： Jian-Ping JIANG Dong-Mei WANG Ting-Jun CHEN Xiao-Long ZHOU Yu-Ping HUO Remi Quirion Yan-Guo HONG College of Life Sciences Fujian Normal University McGill University

Objective The intriguing feature of human Mas oncogene-related G-protein-coupled receptors（Mrg）,also known as sensory neuron-specific receptors,is their exclusive distribution in small-sized neurons in trigeminal and dorsal root ganglia（DRG） in ***,their roles in various types of pain have yet been *** demonstrated that an injection of complete Freund’s adjuvant（CFA） in the hindpaw induced an increase in MrgC receptor mRNA in lumbar *** An intrathecal（i.t.） administration of the selective MrgC receptor agonists,bovine adrenal medulla 8-22（BAM8-22） and（Tyr6）-2-MSH-6-12（MSH）,generated instant short and delayed long-lasting attenuations of CFA-induced thermal *** These effects were associated with the inhibition of upregulations of nNOS and CGRP as well as c-Fos expression in the spinal dorsal horn and/or ***8-22-induced long-lasting anti-hyperalgesia was abolished by an *** of the selective μ-opioid receptor antagonist CTAP（3 nmol）.The ***8-22 also induced increases in mRNAs coding for μ-opioid receptors and proopiomelanocortin（precursor of p-endorphin） as well as p-endorphin content in the lumbar spinal cord and/or DRG in CFA-treated rats.A double labe ling study revealed the co-locahzation of MrgC receptors and nNOS in DRG *** present study suggests that the activation of Mrg receptors can suppress the upregulation of pronociceptive mediators leading to the inhibition of inflammatory *** effects are attributed to the activation of upregulated MrgC receptors and subsequent recruitment of endogenous μ-opioidergic *** The uniquely distributed MrgC receptors could be a novel target for relieving in flammatory pain with minimal CNS unwanted effects.

关键词： Dorsal root ganglia(DRG) inflammatory hyperalgesia Mas-related gene(Mrg) receptors μ-opioid spinal dorsal horn

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