Effects of chronic administration of 7-benzylidene-7-dehydronaltrexone and naltriben on the antinociceptive actions of delta 1- and delta 2-opioid receptor agonists.
Effects of chronic administration of 7-benzylidene-7-dehydronaltrexone and naltriben on the antinociceptive actions of delta 1- and delta 2-opioid receptor agonists.
复制标题
长期服用 7-亚苄基-7-脱氢纳曲酮和纳曲苯对 δ1- 和 δ2-阿片受体激动剂的抗伤害作用的影响。
DOI：
10.1016/0014-2999(96)00411-6
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发表时间：
1996
影响因子：
5
通讯作者：
Thomas,PT
中科院分区：
文献类型：
--
作者：
Bhargava,HN;Zhao,GM;House,RV;Thomas,PT
研究了δ1-阿片受体拮抗剂7-苄基-7-脱氢曲酮和δ2-阿片受体拮抗剂纳曲本分别对小鼠对[d-Pen2， d-Pen5]脑啡肽和[d-Ala2， Glu4deltorphin II， δ1-和δ2-阿片受体激动剂的抗伤害反应的影响。雌性B6C3F1小鼠通过Alzet渗透微型泵皮下植入7-苄基-7-脱氢曲酮（3 mg/kg/d）、硝三苯（1 mg/kg/d）或载药，连续7 d。尾摇试验显示，脑室内注射[d-Pen2， d-Pen5]脑啡肽和[d-Ala2， Glu4]deltorphin II均产生抗伤害感受性，ed50值分别为6.76和6.68 μg/只。长期给药7-苄基-7-脱氢曲酮可降低[d-Pen2， d-Pen5]脑啡肽的ed50，但对[d-Ala2， Glu4]德尔松II的ed50无影响。长期给药硝三苯可降低[d-Ala2， Glu4]deltorphin II的ed50，但对[d-Pen2， d-Pen5]脑啡肽的ed50无影响。[3H][d-Pen2， d-Pen5]脑啡肽与慢性7-苄基-7-脱氢曲酮处理小鼠的全脑膜结合无差异。另一方面，与载药对照组相比，长期服用纳曲本导致[3H][d-Pen2， d-Pen5]脑啡肽结合全脑膜的bmax值轻微但可重复升高。结果表明，长期使用δ1-和δ2-阿片受体拮抗剂分别引起对其激动剂的行为超敏感，进一步证明了δ-阿片受体亚型的存在。
The effects of chronic administration of 7-benzylidene-7-dehydronaltrexone, a δ1-opioid receptor antagonist and naltriben, a δ2-opioid receptor antagonist, on the antinociceptive responses to [d-Pen2, d-Pen5]enkephalin and [d-Ala2, Glu4deltorphin II, δ1- and δ2-opioid receptor agonists, respectively, were determined in the mouse. Female B6C3F1 mice were given 7-benzylidene-7-dehydronaltrexone (3 mg/kg/day), naltriben (1 mg/kg/day) or the vehicle by subcutaneously implanted Alzet osmotic minipumps for 7 days. Both [d-Pen2, d-Pen5]enkephalin and [d-Ala2, Glu4]deltorphin II administered intracerebroventricularly (i.c.v.) produced antinociceptive as measured by the tail-flick test with ED50values of 6.76 and 6.68 μg/mouse, respectively. Chronic administration of 7-benzylidene-7-dehydronaltrexone lowered the ED50of [d-Pen2, d-Pen5]enkephalin but not of [d-Ala2, Glu4]deltorphin II. Chronic administration of naltriben lowered the ED50of [d-Ala2, Glu4]deltorphin II but had no effect on the ED50of [d-Pen2, d-Pen5]enkephalin. The binding of [3H][d-Pen2, d-Pen5]enkephalin to whole brain membranes of chronic 7-benzylidene-7-dehydronaltrexone-treated mice did not differ from chronic vehicle-treated mice. On the other hand, chronic administration of naltriben resulted in slight but reproducible elevation in the Bmaxvalue of [3H][d-Pen2, d-Pen5]enkephalin to bind to whole brain membranes in comparison to vehicle-injected controls. The results suggest that chronic treatment with δ1- and δ2-opioid receptor antagonist cause behavioral supersensitivity to their agonists, respectively, and provides further evidence for the existence of δ-opioid receptor subtypes.