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β-内啡肽是一种强效镇痛剂。

beta-endorphin is a potent analgesic agent.

作者信息

Loh H H, Tseng L F, Wei E, Li C H

出版信息

Proc Natl Acad Sci U S A. 1976 Aug;73(8):2895-8. doi: 10.1073/pnas.73.8.2895.

DOI:10.1073/pnas.73.8.2895
PMID:8780
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC430793/
Abstract

beta-Endorphin, an opiate-like peptide, has potent antinociceptive properties when it is administered directly into the brain and assayed in the the tail-flick, hot-plate, and writhing tests in mice and in the wet shake test in rats. On a molar basis, beta-endorphin is 18 to 33 times more potent than morphine and its actions are blocked by the specific opiate antagonist, naloxone hydrochloride. The activity of beta-endorphin in vivo is also compared to other peptides that show opiate-like activity in assays in vitro.

摘要

β-内啡肽是一种类阿片肽,当直接注入脑内并在小鼠的甩尾试验、热板试验、扭体试验以及大鼠的湿摇试验中进行测定时,它具有强大的抗伤害感受特性。以摩尔为基础计算,β-内啡肽的效力比吗啡强18至33倍,其作用可被特异性阿片拮抗剂盐酸纳洛酮阻断。β-内啡肽在体内的活性也与其他在体外试验中表现出类阿片活性的肽进行了比较。

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1
beta-endorphin is a potent analgesic agent.β-内啡肽是一种强效镇痛剂。
Proc Natl Acad Sci U S A. 1976 Aug;73(8):2895-8. doi: 10.1073/pnas.73.8.2895.
2
Synthesis and analgesic activity of human beta-endorphin.人β-内啡肽的合成与镇痛活性
J Med Chem. 1977 Mar;20(3):325-8. doi: 10.1021/jm00213a001.
3
Stimulation in vivo of the secretion of prolactin and growth hormone by beta-endorphin.
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Endorphins: profound behavioral effects in rats suggest new etiological factors in mental illness.内啡肽:对大鼠产生的显著行为影响提示精神疾病存在新的病因因素。
Science. 1976 Nov 5;194(4265):630-2. doi: 10.1126/science.185694.
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beta-Endorphin: behavioral and analgesic activity in cats.β-内啡肽:猫的行为及镇痛活性
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Spinal action of dermorphin, an extremely potent opioid peptide from frog skin.皮啡肽的脊髓作用,一种来自蛙皮的极其强效的阿片肽。
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本文引用的文献

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Pharmacological effects produced by intracerebral injection of drugs in the conscious mouse.清醒小鼠脑内注射药物所产生的药理效应。
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On the central sites for the antinociceptive action of morphine and fentanyl.关于吗啡和芬太尼抗伤害感受作用的中枢位点。
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New hot plate tests to quantify antinociceptive and narcotic antagonist activities.用于量化抗伤害感受和麻醉拮抗剂活性的新型热板试验。
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Brain sites of precipitated abstinence in morphine-dependent rats.吗啡依赖大鼠中诱发戒断反应的脑区
J Pharmacol Exp Ther. 1973 Apr;185(1):108-15.
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Quantitative aspects of precipitated abstinence in morphine-dependent rats.吗啡依赖大鼠戒断反应的定量研究
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7
Paradoxical effects after microinjection of morphine in the periaqueductal gray matter in the rat.大鼠中脑导水管周围灰质微量注射吗啡后的矛盾效应。
Science. 1974 Sep 20;185(4156):1055-7. doi: 10.1126/science.185.4156.1055.
8
Analgesia and hyperreactivity produced by intracranial microinjections of morphine into the periaqueductal gray matter of the rat.通过向大鼠中脑导水管周围灰质内微量注射吗啡所产生的镇痛和反应过度
Behav Biol. 1974 Jul;11(3):303-13. doi: 10.1016/s0091-6773(74)90548-3.
9
Antagonism of morphine by beta-melanocyte-stimulating hormone and by tetracosactin.β-黑素细胞刺激素和二十四肽促皮质素对吗啡的拮抗作用。
Eur J Pharmacol. 1974 Aug;27(3):339-45. doi: 10.1016/0014-2999(74)90009-0.
10
Antagonism between morphine and the polypeptides ACTH, ACTH1-24 and beta-MSH in the nervous system.吗啡与多肽促肾上腺皮质激素(ACTH)、促肾上腺皮质激素1 - 24(ACTH1 - 24)及β-促黑素细胞激素(β-MSH)在神经系统中的拮抗作用。
Prog Brain Res. 1973;39:383-94. doi: 10.1016/S0079-6123(08)64094-7.