δ-阿片受体拮抗剂纳曲吲哚对成年和幼年大鼠游泳应激诱导的抗伤害感受的拮抗作用。
Antagonism of swim-stress-induced antinociception by the delta-opioid receptor antagonist naltrindole in adult and young rats.
作者信息
Kitchen I, Pinker S R
机构信息
Department of Biochemistry, University of Surrey, Guildford.
出版信息
Br J Pharmacol. 1990 Aug;100(4):685-8. doi: 10.1111/j.1476-5381.1990.tb14076.x.
Abstract
- The availability of the non-peptide delta-opioid receptor antagonist naltrindole has provided the possibility for in vivo studies on the function of delta-opioid receptors. We have studied the effects of naltrindole on swim-stress-induced antinociception in adult and neonatal rats. 2. Adult, 25 and 20 day old rats were stressed by warm water (20 degrees C) swimming for 3 min periods and antinociception was assessed by the tail immersion test (50 degrees C). 3. Naltrindole (0.5 and 1 mg kg-1) antagonized swim-stress-induced antinociception in adult and 25 day old rats but in 20 day old rats naltrindole (1 mg kg-1) was without effect. 4. Antinociception induced by the highly mu-opioid receptor selective agonist alfentanil was completely antagonized by naloxone (1 mg kg-1) but virtually unaffected by naltrindole (1 mg kg-1). 5. Neither naloxone nor naltrindole (1 mg kg-1) antagonized swim-stress-induced rises in plasma corticosterone in adult rats at the time of peak antinociception. 6. In conclusion, naltrindole shows in vivo antagonism of opioid-mediated responses. Swim-stress-induced antinociception is mediated through the delta-opioid receptor in 25 day old and adult rats and through the mu-opioid site in 20 day old animals.
摘要
- 非肽类δ-阿片受体拮抗剂纳曲吲哚的可得性为δ-阿片受体功能的体内研究提供了可能性。我们研究了纳曲吲哚对成年和新生大鼠游泳应激诱导的抗伤害感受的影响。2. 成年大鼠以及25日龄和20日龄的大鼠通过在20℃温水中游泳3分钟进行应激，并用尾浸试验（50℃）评估抗伤害感受。3. 纳曲吲哚（0.5和1mg/kg）拮抗成年和25日龄大鼠游泳应激诱导的抗伤害感受，但在20日龄大鼠中，纳曲吲哚（1mg/kg）无效。4. 高度选择性μ-阿片受体激动剂阿芬太尼诱导的抗伤害感受被纳洛酮（1mg/kg）完全拮抗，但实际上不受纳曲吲哚（1mg/kg）影响。5. 在抗伤害感受达到峰值时，纳洛酮和纳曲吲哚（1mg/kg）均未拮抗成年大鼠游泳应激诱导的血浆皮质酮升高。6. 总之，纳曲吲哚显示出对阿片类介导反应的体内拮抗作用。游泳应激诱导的抗伤害感受在25日龄和成年大鼠中通过δ-阿片受体介导，在20日龄动物中通过μ-阿片位点介导。
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