effects of peripherally acting opioid ligands on central opioid receptors and β-endorphin release in stressed rats影响周边地表演阿片类药物在中枢阿片受体和配体β-endorphin释放在强调老鼠.pdfVIP

Journal of Behavioral and Brain Science, 2012, 2, 162-166 /10.4236/jbbs.2012.22019 Published Online May 2012 (http://www.SciRP.org/journal/jbbs) Effects of Peripherally Acting Opioid Ligands on Central Opioid Receptors and β-Endorphin Release in Stressed Rats * Sergey K. Sudakov , Valentina G. Bashkatova, Tatiyana V. Proskuriakova, Alexey E. Umriukhin P. K. Anokhin Research Institute of Normal Physiology, RAMS, Moscow, Russia * Email: s-sudakov@nphys.ru Received November 18, 2011; revised January 22, 2012; accepted February 22, 2012 ABSTRACT 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