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多种阿片受体:酒精选择性抑制与δ受体的结合。

Multiple opiate receptors: alcohol selectively inhibits binding to delta receptors.

作者信息

Hiller J M, Angel L M, Simon E J

出版信息

Science. 1981 Oct 23;214(4519):468-9. doi: 10.1126/science.6270788.

DOI:10.1126/science.6270788
PMID:6270788
Abstract

The addition of ethanol or other aliphatic alcohols to rat brain membranes strongly inhibits binding of enkephalins at concentrations at which little inhibition of opiate alkaloids is seen. Inhibition is reversible, and potency increases with chain length of the alcohol. The results suggest that delta receptors are considerably more sensitive to alcohols than mu receptors. This is the first demonstration of selective inhibition of one of the postulated classes of opiate receptors by a reagent that is not a ligand for the receptor.

摘要

向大鼠脑膜中添加乙醇或其他脂肪醇,在对阿片生物碱几乎没有抑制作用的浓度下,能强烈抑制脑啡肽的结合。抑制作用是可逆的,且效力随醇链长度增加而增强。结果表明,δ受体对醇的敏感性远高于μ受体。这是首次证明一种并非受体配体的试剂对假定的阿片受体类别之一具有选择性抑制作用。

相似文献

1
Multiple opiate receptors: alcohol selectively inhibits binding to delta receptors.多种阿片受体:酒精选择性抑制与δ受体的结合。
Science. 1981 Oct 23;214(4519):468-9. doi: 10.1126/science.6270788.
2
Characterization of the selective inhibition of the delta subclass of opioid binding sites by alcohols.酒精对阿片样物质结合位点δ亚类的选择性抑制作用的表征。
Mol Pharmacol. 1984 Mar;25(2):249-55.
3
Opiate receptor binding characteristics of dimeric analogues of mu-selective DAGO-enkephalin.μ-选择性DAGO-脑啡肽二聚体类似物的阿片受体结合特性
Biochem Int. 1986 Aug;13(2):199-203.
4
Sodium regulation of agonist binding at opioid receptors. I. Effects of sodium replacement on binding at mu- and delta-type receptors in 7315c and NG108-15 cells and cell membranes.阿片受体激动剂结合的钠调节。I. 钠替代对7315c和NG108-15细胞及细胞膜中μ型和δ型受体结合的影响。
Mol Pharmacol. 1986 Aug;30(2):81-9.
5
Dehydro-enkephalins. IV. Discriminative recognition of delta and mu opiate receptors by enkephalin analogs.脱氢脑啡肽。IV. 脑啡肽类似物对δ和μ阿片受体的鉴别性识别。
Biochem Biophys Res Commun. 1982 Jan 29;104(2):583-90. doi: 10.1016/0006-291x(82)90677-5.
6
Molecular mechanisms of ligand binding to opioid receptors: selective inhibition by ethanol?配体与阿片受体结合的分子机制:乙醇的选择性抑制作用?
NIDA Res Monogr. 1986;75:355-8.
7
Down regulation of enkephalin (delta) receptors. Demonstration in membrane-bound and solubilized receptors.
Biochim Biophys Acta. 1982 Dec 30;721(4):478-84. doi: 10.1016/0167-4889(82)90104-5.
8
Characterization of [3H][2-D-penicillamine, 5-D-penicillamine]-enkephalin binding to delta opiate receptors in the rat brain and neuroblastoma--glioma hybrid cell line (NG 108-15).[3H][2-D-青霉胺,5-D-青霉胺]脑啡肽与大鼠脑及神经母细胞瘤-胶质瘤杂交细胞系(NG 108-15)中δ阿片受体结合的特性研究
Proc Natl Acad Sci U S A. 1985 Apr;82(8):2543-7. doi: 10.1073/pnas.82.8.2543.
9
Possible role of distinct morphine and enkephalin receptors in mediating actins of benzomorphan drugs (putative kappa and sigma agonists).不同的吗啡和脑啡肽受体在介导苯并吗啡烷类药物(假定的κ和σ激动剂)作用中的可能作用。
Proc Natl Acad Sci U S A. 1980 Aug;77(8):4469-73. doi: 10.1073/pnas.77.8.4469.
10
Opioid receptors in human neuroblastoma SH-SY5Y cells: evidence for distinct morphine (mu) and enkephalin (delta) binding sites.人神经母细胞瘤SH-SY5Y细胞中的阿片受体:不同的吗啡(μ)和脑啡肽(δ)结合位点的证据。
Biochem Biophys Res Commun. 1986 Jun 13;137(2):813-20. doi: 10.1016/0006-291x(86)91152-6.

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Sleep and the Pharmacotherapy of Alcohol Use Disorder: Unfortunate Bedfellows. A Systematic Review With Meta-Analysis.睡眠与酒精使用障碍的药物治疗:不幸的伙伴。一项系统评价与荟萃分析
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3
Testosterone modulation of ethanol effects on the µ-opioid receptor kinetics in castrated rats.
睾酮对去势大鼠乙醇作用于μ-阿片受体动力学的调节
Biomed Rep. 2019 Sep;11(3):103-109. doi: 10.3892/br.2019.1230. Epub 2019 Jul 18.
4
Pharmacotherapy of alcohol use disorders: seventy-five years of progress.酒精使用障碍的药物治疗:75年的进展
J Stud Alcohol Drugs Suppl. 2014;75(17):79-88. doi: 10.15288/jsads.2014.s17.79.
5
Influence of the endogenous opioid system on high alcohol consumption and genetic predisposition to alcoholism.内源性阿片系统对高酒精摄入量及酒精成瘾遗传易感性的影响。
J Psychiatry Neurosci. 2001 Sep;26(4):304-18.
6
Genetics of alcoholism: role of the endogenous opioid system.酒精中毒的遗传学:内源性阿片系统的作用。
Metab Brain Dis. 1994 Jun;9(2):105-31. doi: 10.1007/BF01999765.
7
Endogenous opioids and excessive alcohol consumption.内源性阿片类物质与过度饮酒。
J Psychiatry Neurosci. 1993 Jul;18(4):148-56.
8
Multiple effects of short-chain alcohols on binding to rat heart muscarinic receptors.短链醇对大鼠心脏毒蕈碱受体结合的多种作用。
Biochem J. 1984 Apr 15;219(2):563-71. doi: 10.1042/bj2190563.
9
Naloxone reduces diuretic responses induced by water, alcohol or congenital lack of vasopressin in rats.纳洛酮可降低水、酒精或先天性抗利尿激素缺乏诱导的大鼠利尿反应。
Br J Pharmacol. 1984 Jan;81(1):85-90. doi: 10.1111/j.1476-5381.1984.tb10747.x.
10
Ethanol acceptance as a function of genotype amounts of brain [Met]enkephalin.乙醇接受量作为脑内[甲硫氨酸]脑啡肽基因型数量的函数。
Proc Natl Acad Sci U S A. 1983 Nov;80(21):6510-2. doi: 10.1073/pnas.80.21.6510.