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纳洛酮不可逆应激诱导镇痛后μ阿片受体拮抗剂的镇痛作用

Analgesic effects of mu antagonists after naloxone non-reversible stress-induced analgesia.

作者信息

Sacerdote P, Mantegazza P, Panerai A E

出版信息

Brain Res. 1985 Dec 16;359(1-2):34-8. doi: 10.1016/0006-8993(85)91409-x.

DOI:10.1016/0006-8993(85)91409-x
PMID:3000523
Abstract

Three antagonists at the mu opiate receptor site: naloxone, naltrexone and diprenorphine, and one agonist-antagonist compound nalorphine, at doses usually not analgesic elicited analgesia in rats when administered after non-naloxone-reversible shock-induced analgesia had disappeared. The chi receptor antagonist, MR 2266, and the delta antagonist, ICI 154129, were all ineffective. This effect was no longer present when non-naloxone-reversible shock-induced analgesia was inhibited by the administration of the chi receptor antagonist, MR 2266. These results suggest that the mu opiate receptor may change its conformation under particular conditions such as continuous inescapable shock.

摘要

三种μ阿片受体位点拮抗剂:纳洛酮、纳曲酮和二丙诺啡,以及一种激动剂 - 拮抗剂化合物烯丙吗啡,在非纳洛酮可逆性休克诱导的镇痛作用消失后给药时,通常无镇痛作用的剂量在大鼠中引发了镇痛作用。κ受体拮抗剂MR 2266和δ拮抗剂ICI 154129均无效。当通过给予κ受体拮抗剂MR 2266抑制非纳洛酮可逆性休克诱导的镇痛作用时,这种效应不再出现。这些结果表明,μ阿片受体可能在特定条件下(如持续不可逃避的休克)改变其构象。

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1
Analgesic effects of mu antagonists after naloxone non-reversible stress-induced analgesia.纳洛酮不可逆应激诱导镇痛后μ阿片受体拮抗剂的镇痛作用
Brain Res. 1985 Dec 16;359(1-2):34-8. doi: 10.1016/0006-8993(85)91409-x.
2
Opiate antagonists and long-term analgesic reaction induced by inescapable shock in rats.
J Comp Physiol Psychol. 1980 Dec;94(6):1172-83. doi: 10.1037/h0077743.
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Nalorphine as a stimulus in drug discrimination learning: assessment of the role of mu- and kappa-receptor subtypes.纳洛啡作为药物辨别学习中的刺激物:μ和κ受体亚型作用的评估
Pharmacol Biochem Behav. 1994 Jul;48(3):635-42. doi: 10.1016/0091-3057(94)90325-5.
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Relative involvement of mu, kappa and delta receptor mechanisms in opiate-mediated antinociception in mice.μ、κ和δ受体机制在阿片介导的小鼠抗伤害感受中的相对参与情况。
J Pharmacol Exp Ther. 1983 Mar;224(3):525-30.
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The effects of mu, delta- and kappa-opioid receptor antagonists on the pain threshold increase following muscle stimulation in the rat.μ、δ和κ阿片受体拮抗剂对大鼠肌肉刺激后痛阈升高的影响。
Acta Physiol Scand. 1990 Nov;140(3):353-8. doi: 10.1111/j.1748-1716.1990.tb09009.x.
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Kappa-receptor antagonist reverse 'non-opioid' stress-induced analgesia.
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Extent and control of shock affects naltrexone sensitivity of stress-induced analgesia and reactivity to morphine.休克的程度和控制会影响应激诱导镇痛的纳曲酮敏感性以及对吗啡的反应性。
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Different opioid systems may participate in post-electro-convulsive shock (ECS) analgesia and catalepsy.不同的阿片系统可能参与电惊厥休克(ECS)后的镇痛和僵住症。
Brain Res. 1981 Aug 31;219(2):385-96. doi: 10.1016/0006-8993(81)90301-2.

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