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β-内啡肽-（1-27）是β-内啡肽镇痛的拮抗剂。

beta-endorphin-(1-27) is an antagonist of beta-endorphin analgesia.

作者信息

Hammonds R G, Nicolas P, Li C H

出版信息

Proc Natl Acad Sci U S A. 1984 Mar;81(5):1389-90. doi: 10.1073/pnas.81.5.1389.

DOI:10.1073/pnas.81.5.1389
PMID:6324189
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC344839/
Abstract

beta h-Endorphin-(1-27), a naturally occurring fragment of human beta-endorphin (beta h-endorphin), diminishes the analgesic effect of beta h-endorphin when coinjected intra-cerebroventricularly into mice. A parallel shift in the dose-response curve of beta h-endorphin in the presence of beta h-endorphin-(1-27) suggests competition at the same site. The potency of beta h-endorphin-(1-27) in antagonizing analgesia is greater than 4 times greater than that of the opiate antagonist naloxone.

摘要

βh-内啡肽-（1-27）是人类β-内啡肽（βh-内啡肽）的一种天然存在的片段，当与βh-内啡肽共同脑室内注射到小鼠体内时，会减弱βh-内啡肽的镇痛作用。在存在βh-内啡肽-（1-27）的情况下，βh-内啡肽剂量-反应曲线的平行移动表明在同一部位存在竞争。βh-内啡肽-（1-27）拮抗镇痛的效力比阿片拮抗剂纳洛酮的效力大4倍以上。

相似文献

1
beta-endorphin-(1-27) is an antagonist of beta-endorphin analgesia.β-内啡肽-（1-27）是β-内啡肽镇痛的拮抗剂。
Proc Natl Acad Sci U S A. 1984 Mar;81(5):1389-90. doi: 10.1073/pnas.81.5.1389.
2
Beta-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia.β-内啡肽-（1-27）是依托啡肽诱导镇痛的天然拮抗剂。
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beta-Endorphin-induced analgesia is inhibited by synthetic analogs of beta-endorphin.β-内啡肽诱导的镇痛作用受到β-内啡肽合成类似物的抑制。
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Inhibition of analgesia by C-terminal deletion analogs of human beta-endorphin.人β-内啡肽C末端缺失类似物对镇痛作用的抑制
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Roles of β-Endorphin in Stress, Behavior, Neuroinflammation, and Brain Energy Metabolism.β-内啡肽在应激、行为、神经炎症和大脑能量代谢中的作用。
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beta-Endorphin-induced analgesia is inhibited by synthetic analogs of beta-endorphin.β-内啡肽诱导的镇痛作用受到β-内啡肽合成类似物的抑制。
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本文引用的文献

1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
Beta-Endorphin: synthesis and radioreceptor binding activity of Beta h-endorphin-(1-27) and its analogs.β-内啡肽：βh-内啡肽-（1-27）及其类似物的合成与放射受体结合活性
Int J Pept Protein Res. 1981 Mar;17(3):292-6. doi: 10.1111/j.1399-3011.1981.tb01995.x.
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beta-Endorphin and related peptides in pituitary, brain, pancreas and antrum.垂体、脑、胰腺和胃窦中的β-内啡肽及相关肽。
Br Med Bull. 1983 Jan;39(1):25-30. doi: 10.1093/oxfordjournals.bmb.a071786.
4
Binding of 3H-beta-endorphin in rat brain.3H-β-内啡肽在大鼠脑中的结合
Life Sci. 1982;31(12-13):1381-4. doi: 10.1016/0024-3205(82)90386-1.
5
beta-Endorphin: analgesic and receptor binding activity of non-mammalian homologs.β-内啡肽：非哺乳动物同源物的镇痛及受体结合活性
Int J Pept Protein Res. 1982 May;19(5):556-61. doi: 10.1111/j.1399-3011.1982.tb02642.x.
6
Beta-endorphin: opiate receptor binding activities of six naturally occurring beta-endorphin homologs studied by using tritiated human hormone and naloxone as primary ligands--effects of sodium ion.β-内啡肽：以氚标记的人激素和纳洛酮作为主要配体研究六种天然存在的β-内啡肽同系物的阿片受体结合活性——钠离子的影响
Proc Natl Acad Sci U S A. 1982 Apr;79(7):2191-3. doi: 10.1073/pnas.79.7.2191.
7
Isolation and properties of beta-endorphin-(1-27), N alpha-acetyl-beta-endorphin, corticotropin, gamma-lipotropin and neurophysin from equine pituitary glands.从马垂体中分离出β-内啡肽-（1-27）、Nα-乙酰-β-内啡肽、促肾上腺皮质激素、γ-促脂素和神经垂体素及其性质
Int J Pept Protein Res. 1981 Nov;18(5):443-50. doi: 10.1111/j.1399-3011.1981.tb03005.x.
8
beta-Endorphin- (1-27): acetylation of alpha-amino groups enhances immunoreactivity but diminishes analgesic and receptor-binding activities with no changes in circular dichroism spectra.β-内啡肽-（1-27）：α-氨基的乙酰化增强免疫反应性，但会降低镇痛和受体结合活性，而圆二色光谱无变化。
Biochem Biophys Res Commun. 1980 Dec 16;97(3):932-8. doi: 10.1016/0006-291x(80)91466-7.
9
Peptide inhibitor of morphine- and beta-endorphin-induced analgesia.吗啡和β-内啡肽诱导镇痛的肽类抑制剂。
Proc Natl Acad Sci U S A. 1980 Sep;77(9):5525-6. doi: 10.1073/pnas.77.9.5525.
10
Quantitative studies of the antagonism of morphine by nalorphine and naloxone.纳洛芬和纳洛酮对吗啡拮抗作用的定量研究。
J Pharmacol Exp Ther. 1969 Sep;169(1):39-45.