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
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.
作者信息
Nicolas P, Hammonds R G, Li C H
出版信息
Proc Natl Acad Sci U S A. 1982 Apr;79(7):2191-3. doi: 10.1073/pnas.79.7.2191.
Abstract
Six naturally occurring homologs of beta-endorphin were tested for their potency in inhibiting the binding of [3H]naloxone and [3H]-beta h-endorphin either in the presence or in the absence of Na+. Sodium ion reduces inhibitory potency of these homologs against [3H]-beta h-endorphin and [3H]naloxone to about the same extent. The ratio of the IC50 obtained with Na+ to that obtained without Na+ is not highly correlated with analgesic potency. Very high (greater than 300) sodium ratios are observed with some homologs. A significant rank correlation was found between the ratio of the relative potency in displacing [3H]beta h-endorphin to the relative potency in analgesia and potency in inhibiting the binding of the pure antagonist naloxone.
摘要
对β-内啡肽的六种天然存在的同系物进行了测试，以考察它们在存在或不存在Na+的情况下抑制[3H]纳洛酮和[3H]-βh-内啡肽结合的效力。钠离子使这些同系物对[3H]-βh-内啡肽和[3H]纳洛酮的抑制效力降低到大致相同的程度。有Na+时获得的IC50与无Na+时获得的IC50之比与镇痛效力没有高度相关性。在一些同系物中观察到非常高（大于300）的钠比。在置换[3H]βh-内啡肽的相对效力与镇痛相对效力之比以及抑制纯拮抗剂纳洛酮结合的效力之间发现了显著的等级相关性。
相似文献
1
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.
2
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.
3
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.
4
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。
Proc Natl Acad Sci U S A. 1985 May;82(10):3178-81. doi: 10.1073/pnas.82.10.3178.
5
Binding of 3H-beta-endorphin to rat brain membranes: characterization of opiate properties and interaction with ACTH.3H-β-内啡肽与大鼠脑膜的结合：阿片样物质特性及其与促肾上腺皮质激素相互作用的表征
Eur J Pharmacol. 1980 May 30;64(1):1-8. doi: 10.1016/0014-2999(80)90363-5.
6
Differential effect of humoral endorphin on the binding of opiate agonists and antagonists.体液内啡肽对阿片激动剂和拮抗剂结合的差异效应。
Eur J Pharmacol. 1982 Jul 9;81(2):227-35. doi: 10.1016/0014-2999(82)90440-x.
7
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。
Proc Natl Acad Sci U S A. 1984 May;81(10):3074-7. doi: 10.1073/pnas.81.10.3074.
8
[Comparative activity of endorphins on the opiate receptors].[内啡肽对阿片受体的比较活性]
C R Acad Hebd Seances Acad Sci D. 1977 Jul 18;285(3):257-60.
9
Use of 125I-Tyr27 beta-endorphin for the study of beta-endorphin binding sites in rat cortex.使用¹²⁵I-酪氨酰²⁷β-内啡肽研究大鼠皮层中的β-内啡肽结合位点。
Neuroendocrinology. 1986;43(6):629-34. doi: 10.1159/000124592.
10
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
Biochem Biophys Res Commun. 1985 Mar 15;127(2):649-55. doi: 10.1016/s0006-291x(85)80210-2.
引用本文的文献
1
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。
Proc Natl Acad Sci U S A. 1984 May;81(10):3074-7. doi: 10.1073/pnas.81.10.3074.
2
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.
3
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。
Proc Natl Acad Sci U S A. 1985 May;82(10):3178-81. doi: 10.1073/pnas.82.10.3178.
本文引用的文献
1
A modification of receptor theory.受体理论的一种修正。
Br J Pharmacol Chemother. 1956 Dec;11(4):379-93. doi: 10.1111/j.1476-5381.1956.tb00006.x.
2
3
Beta-Endorphin. Synthesis and radioreceptor-binding activity of the ostrich hormone.β-内啡肽。鸵鸟激素的合成与放射受体结合活性。
Int J Pept Protein Res. 1982 Mar;19(3):251-3.
4
beta-Endorphin: isolation, amino acid sequence and synthesis of the hormone from horse pituitary glands.β-内啡肽：从马垂体中分离、氨基酸序列及该激素的合成。
Int J Pept Protein Res. 1981 Sep;18(3):242-8. doi: 10.1111/j.1399-3011.1981.tb02978.x.
5
Beta-endorphin: replacement of tyrosine in position 27 by tryptophan increases analgesic potency--preparation and properties of the 2-nitrophenylsulfenyl derivative.β-内啡肽：27位酪氨酸被色氨酸取代可增强镇痛效力——2-硝基苯基亚磺酰衍生物的制备及性质
Proc Natl Acad Sci U S A. 1982 Feb;79(4):1042-4. doi: 10.1073/pnas.79.4.1042.
6
Interaction of tritiated beta-endorphin with rat brain membranes.氚标记的β-内啡肽与大鼠脑膜的相互作用。
Anal Biochem. 1981 Jun;114(1):75-84. doi: 10.1016/0003-2697(81)90454-1.
7
Synthesis and radioreceptor binding activity of turkey beta-endorphin and deacetylated salmon endorphin.火鸡β-内啡肽和去乙酰化鲑鱼内啡肽的合成及放射受体结合活性
Int J Pept Protein Res. 1980 Jul;16(1):75-8. doi: 10.1111/j.1399-3011.1980.tb02938.x.
8
beta-Endorphin: radioreceptor binding assay. Relative potency of synthetic analogs with various chain lengths.β-内啡肽：放射受体结合测定。不同链长合成类似物的相对效价。
Int J Pept Protein Res. 1980 Jul;16(1):66-9.
9
beta-Endorphin omission analogs: dissociation of immunoreactivity from other biological activities.β-内啡肽缺失类似物：免疫反应性与其他生物学活性的解离
Proc Natl Acad Sci U S A. 1980 Jun;77(6):3211-4. doi: 10.1073/pnas.77.6.3211.
10
Beta-Endorphin: dissociation of receptor binding activity from analgesic potency.β-内啡肽：受体结合活性与镇痛效力的解离。
Proc Natl Acad Sci U S A. 1980 Apr;77(4):2303-4. doi: 10.1073/pnas.77.4.2303.
Zotero 插件