D'Addario Claudio, Di Benedetto Manuela, Izenwasser Sari, Candeletti Sanzio, Romualdi Patrizia
Department of Pharmacology, University of Bologna, 40126 Bologna, Italy.
J Mol Neurosci. 2004;24(2):307-14. doi: 10.1385/JMN:24:2:307.
The effects of kappa-opioid agonist treatment on kappa-opioid receptor density and on dynorphin A levels in the rat brain were studied. Rats were treated with the selective kappa-opioid agonist U-69593 or vehicle for 5 d. Dynorphin A levels and kappa-opioid receptor binding were measured on day 8 (3 d after the last injection) or 22 (17 d after the last injection). On day 8, kappa-opioid receptor density was increased in the hypothalamus of rats treated with U-69593; there were no changes in the frontal cortex or caudate putamen. In contrast, there was an increase in dynorphin A levels in the frontal cortex and no changes in hypothalamus and caudate putamen in response to U-69593. On day 22, Bmax was decreased in frontal cortex and caudate putamen of U-69593-treated rats, whereas dynorphin A levels were increased in the caudate putamen and in the frontal cortex. These findings suggest that kappa-opioid receptor agonist treatment has long-term, continually changing effects on the kappa-opioid system.
研究了κ-阿片受体激动剂治疗对大鼠脑内κ-阿片受体密度和强啡肽A水平的影响。用选择性κ-阿片受体激动剂U-69593或赋形剂处理大鼠5天。在第8天（最后一次注射后3天）或第22天（最后一次注射后17天）测量强啡肽A水平和κ-阿片受体结合情况。在第8天，用U-69593处理的大鼠下丘脑内κ-阿片受体密度增加；额叶皮质或尾状壳核无变化。相反，对U-69593的反应是额叶皮质中强啡肽A水平增加，而下丘脑和尾状壳核无变化。在第22天，U-69593处理的大鼠额叶皮质和尾状壳核中的Bmax降低，而尾状壳核和额叶皮质中的强啡肽A水平增加。这些发现表明，κ-阿片受体激动剂治疗对κ-阿片系统具有长期的、不断变化的影响。
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