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μ、κ和δ受体激动剂暴露后家兔空肠急性阿片类药物戒断挛缩的表现。

Manifestations of acute opiate withdrawal contracture in rabbit jejunum after mu-, kappa- and delta-receptor agonist exposure.

作者信息

Valeri P, Morrone L A, Romanelli L

机构信息

Institute of Pharmacology and Pharmacognosy, University of Rome La Sapienza, Italy.

出版信息

Br J Pharmacol. 1992 May;106(1):39-44. doi: 10.1111/j.1476-5381.1992.tb14289.x.

DOI:10.1111/j.1476-5381.1992.tb14289.x
PMID:1354541
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1907462/
Abstract
  1. Following a 5 min in vitro exposure to morphine (1.3 x 10(-7) M), U-50,488H (2.5 x 10(-8) M) and deltorphin (1.6 x 10(-8)-6.5 x 10(-9) M), the rabbit isolated jejunum exhibited a precipitated contracture after the addition of naloxone (2.75 x 10(-7) M). 2. The precipitated responses to U-50,488H and deltorphin but not to morphine were reproducible in the same tissue. 3. The precipitated contractures were blocked completely by tetrodotoxin (3 x 10(-7) M), partially by atropine (1.5 x 10(-7) M) and not affected by hexamethonium (1.4 x 10(-5) M). 4. Naloxone administration (2.75 x 10(-7) M) before the agonist prevented the development of the adaptive response to morphine and U-50,488H but not to deltorphin. 5. The selective antagonists norbinaltorphimine (2.7 x 10(-8)-2.7 x 10(-9) M) and naltrindole (1.1 x 10(-7) M) prevented the adaptive response development only to the respective agonists. 6. The opioid agonists partially inhibited the spontaneous activity of the tissue. This study has shown that independent activation of mu-, kappa- and delta-opioid receptors can induce dependence in this isolated tissue. Rabbit jejunum is a suitable tissue for studying the acute effects of opioids on the adaptative processes determined by their administration.
摘要
  1. 在兔离体空肠体外暴露于吗啡(1.3×10⁻⁷M)、U - 50,488H(2.5×10⁻⁸M)和强啡肽(1.6×10⁻⁸ - 6.5×10⁻⁹M)5分钟后,加入纳洛酮(2.75×10⁻⁷M)会引起空肠出现沉淀性挛缩。2. 对U - 50,488H和强啡肽而非吗啡产生的沉淀反应在同一组织中可重现。3. 沉淀性挛缩被河豚毒素(3×10⁻⁷M)完全阻断,被阿托品(1.5×10⁻⁷M)部分阻断,且不受六甲铵(1.4×10⁻⁵M)影响。4. 在给予激动剂前给予纳洛酮(2.75×10⁻⁷M)可阻止对吗啡和U - 50,488H的适应性反应的发展,但不能阻止对强啡肽的适应性反应。5. 选择性拮抗剂去甲丙氧芬(2.7×10⁻⁸ - 2.7×10⁻⁹M)和纳曲吲哚(1.1×10⁻⁷M)仅能阻止对各自激动剂的适应性反应的发展。6. 阿片类激动剂部分抑制组织的自发活动。本研究表明,μ-、κ-和δ-阿片受体的独立激活可在该离体组织中诱导依赖性。兔空肠是研究阿片类药物对其给药所决定的适应性过程的急性影响的合适组织。

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本文引用的文献

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Model of opiate dependence in the guinea-pig isolated ileum.豚鼠离体回肠阿片类药物依赖模型。
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Pharmacological characterization of opiate physical dependence in the isolated ileum of the guinea-pig.豚鼠离体回肠中阿片类物质身体依赖性的药理学特性
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Opioid binding properties of brain and peripheral tissues: evidence for heterogeneity in opioid ligand binding sites.脑和外周组织的阿片样物质结合特性:阿片样物质配体结合位点存在异质性的证据。
J Pharmacol Exp Ther. 1980 Aug;214(2):395-402.
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Enkephalin receptor in the rabbit ileum.兔回肠中的脑啡肽受体。
Br J Pharmacol. 1980 Feb;68(2):193-5. doi: 10.1111/j.1476-5381.1980.tb10406.x.
8
Pharmacological characterization of the inhibitory effects of neurotensin on the rabbit ileum myenteric plexus preparation.神经降压素对兔回肠肌间神经丛标本抑制作用的药理学特性
Br J Pharmacol. 1983 Dec;80(4):645-53. doi: 10.1111/j.1476-5381.1983.tb10054.x.
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U-50,488: a selective and structurally novel non-Mu (kappa) opioid agonist.U-50,488:一种具有选择性且结构新颖的非μ(κ)阿片类激动剂。
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