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首页> 外文期刊>Life sciences >Possible involvement of mu(1)-opioid receptors in the fentanyl- or morphine-induced antinociception at supraspinal and spinal sites
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Possible involvement of mu(1)-opioid receptors in the fentanyl- or morphine-induced antinociception at supraspinal and spinal sites

机译：mu（1）-阿片受体可能参与了上脊髓和脊髓上的芬太尼或吗啡诱导的抗伤害感受

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Fentanyl has been shown to be a potent analgesic with a lower propensity to produce tolerance and physical dependence in the clinical setting. The present study was designed to investigate the mechanisms of fentanyl- or morphine-induced antinociception at both supraspinal and spinal sites. In the mouse tail-flick test, the antinociceptive effects induced by both fentanyl and morphine were blocked by either the mu(1)-opioid receptor antagonist naloxonazine or the mu(1)/mu(2)-opioid receptor antagonist beta-funaltrexamine (beta-FNA) after s.c., i.c.v. or i.t. injection. In contrast, both fentanyl and morphine given i.c.v. or i.t. failed to produce antinociception in mu(1)-deficient CXBK mice. These findings indicate that like morphine, the antinociception induced by fentanyl may be mediated predominantly through mu(1)-opioid receptors at both supraspinal and spinal sites in mice. We also determined the ED50 values for s.c.-, i.c.v.- and i.t.-administered fentanyl- or morphine-induced antinociception in mice. The ED50 values for s.c.-, i.c.v.- and i.t.-administered fentanyl-induced antinociception were 73.7, 18.5 and 1.2-fold lower than that of morphine, respectively. The present data clearly suggest the usefulness of peripheral treatment with fentanyl for the control of pain. (C) 2002 Elsevier Science Inc. All rights reserved. [References: 15]
机译：芬太尼已被证明是一种有效的镇痛药，在临床环境中具有较低的产生耐受性和身体依赖性的倾向。本研究旨在研究芬太尼或吗啡诱导的脊髓上和脊髓部位抗伤害感受的机制。在小鼠甩尾试验中，由mu（1）-阿片类受体拮抗剂纳洛酮嗪或mu（1）/ mu（2）-阿片类受体拮抗剂β-富勒烯胺（）阻断了芬太尼和吗啡诱导的抗伤害作用beta，FNA）后，sc，icv或注射。相比之下，芬太尼和吗啡在静脉内给药。或未能在mu（1）缺乏CXBK小鼠中产生抗伤害感受。这些发现表明，与吗啡一样，芬太尼诱导的抗伤害感受作用可能主要通过小鼠脊髓上和脊髓部位的mu（1）-阿片样物质受体介导。我们还确定了皮下注射芬太尼或吗啡诱导的抗伤害感受的s.c .-，i.c.v.-和i.t.的ED50值。皮下注射芬太尼诱导的抗伤害感受的s.c .-，i.c.v.-和i.t.的ED50值分别比吗啡低73.7、18.5和1.2倍。本数据清楚地表明用芬太尼进行外周治疗可有效控制疼痛。 （C）2002 Elsevier Science Inc.保留所有权利。 [参考：15]

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