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1
Bronchial and vascular effects of Paf in the rat isolated lung are completely blocked by WEB 2086, a novel specific Paf antagonist.新型特异性血小板活化因子（PAF）拮抗剂WEB 2086可完全阻断PAF对大鼠离体肺支气管和血管的作用。
Br J Pharmacol. 1987 Aug;91(4):799-802. doi: 10.1111/j.1476-5381.1987.tb11278.x.
2
Inhibitor effect of apafant on bronchopulmonary responses to platelet activating factor and to antigen in rats.阿帕泛对大鼠支气管肺脏对血小板活化因子及抗原反应的抑制作用。
Arzneimittelforschung. 1997 Dec;47(12):1364-9.
3
Limited interference of specific Paf antagonists with hyper-responsiveness to Paf itself of lungs from actively sensitized guinea-pigs.特定血小板活化因子拮抗剂对主动致敏豚鼠肺脏对血小板活化因子自身高反应性的有限干扰。
Br J Pharmacol. 1989 Jun;97(2):433-42. doi: 10.1111/j.1476-5381.1989.tb11970.x.
4
The action of platelet activating factor and its antagonism by WEB 2086 on human isolated airways.
Eur Respir J. 1990 Jan;3(1):55-60.
5
PAF potentiates protamine-induced lung edema: role of pulmonary venoconstriction.血小板活化因子增强鱼精蛋白诱导的肺水肿：肺静脉收缩的作用
J Appl Physiol (1985). 1990 Mar;68(3):1059-68. doi: 10.1152/jappl.1990.68.3.1059.
6
Effect of a Paf antagonist, WEB 2086, on airway microvascular leakage in the guinea-pig and platelet aggregation in man.血小板激活因子拮抗剂WEB 2086对豚鼠气道微血管渗漏及人血小板聚集的影响。
Br J Pharmacol. 1988 May;94(1):164-8. doi: 10.1111/j.1476-5381.1988.tb11511.x.
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Platelet-activating factor (Paf) antagonist, WEB 2086, protects against Paf-induced hypotension in Macaca fascicularis.血小板活化因子（PAF）拮抗剂WEB 2086可保护猕猴免受PAF诱导的低血压影响。
Br J Pharmacol. 1989 Jul;97(3):643-6. doi: 10.1111/j.1476-5381.1989.tb11999.x.
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Pulmonary vascular reactivity: effect of PAF and PAF antagonists.肺血管反应性：血小板活化因子及血小板活化因子拮抗剂的作用
J Appl Physiol (1985). 1992 Nov;73(5):1762-9. doi: 10.1152/jappl.1992.73.5.1762.
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Pulmonary hypertension and edema induced by platelet-activating factor in isolated, perfused rat lungs are blocked by BN52021.
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Effects of endothelin-1 on vascular permeability in the conscious rat: interactions with platelet-activating factor.内皮素-1对清醒大鼠血管通透性的影响：与血小板活化因子的相互作用。
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1
Macrophage VLDL receptor promotes PAFAH secretion in mother's milk and suppresses systemic inflammation in nursing neonates.巨噬细胞 VLDL 受体促进母乳中 PAFAH 的分泌，并抑制哺乳期新生儿的全身炎症。
Nat Commun. 2012;3:1008. doi: 10.1038/ncomms2011.
2
Bacteria induce release of platelet-activating factor (PAF) from polymorphonuclear neutrophil granulocytes: possible role for PAF in pathogenesis of experimentally induced bacterial pneumonia.细菌诱导多形核中性粒细胞释放血小板活化因子（PAF）：PAF在实验性诱导的细菌性肺炎发病机制中的可能作用。
Infect Immun. 1993 May;61(5):1996-2002. doi: 10.1128/iai.61.5.1996-2002.1993.
3
Interaction of the Paf antagonist WEB 2086 and its hetrazepine analogues with human platelets and endothelial cells.血小板活化因子拮抗剂WEB 2086及其杂氮䓬类似物与人类血小板和内皮细胞的相互作用。
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Effect of platelet-activating factor on porcine pulmonary blood vessels in vitro.血小板活化因子对猪肺血管的体外作用
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Thieno-triazolo-1,4-diazepines as antagonists of platelet-activating factor: present status.噻吩并三唑并-1,4-二氮杂䓬类作为血小板活化因子拮抗剂：现状
Lipids. 1991 Dec;26(12):1157-61. doi: 10.1007/BF02536522.

本文引用的文献

1
Differential effects of platelet depletion on the physiologic alterations of IgE anaphylaxis and acetyl glyceryl ether phosphorylcholine infusion in the rabbit.血小板减少对兔IgE过敏反应和乙酰甘油醚磷酸胆碱输注的生理改变的不同影响。
Am Rev Respir Dis. 1981 Oct;124(4):416-21. doi: 10.1164/arrd.1981.124.4.416.
2
Nonimmunological production of leukotrienes induced by platelet-activating factor.血小板活化因子诱导的白三烯非免疫性产生
Science. 1982 Oct 15;218(4569):286-9. doi: 10.1126/science.7123233.
3
Platelet-activating factor increases pulmonary microvascular permeability and induces pulmonary edema. A preliminary report.血小板活化因子增加肺微血管通透性并诱发肺水肿。初步报告。
Bull Eur Physiopathol Respir. 1983 May-Jun;19(3):253-6.
4
Acute effects of intratracheal administration of platelet-activating factor in baboons.气管内给予狒狒血小板活化因子的急性效应。
J Appl Physiol Respir Environ Exerc Physiol. 1983 Sep;55(3):799-804. doi: 10.1152/jappl.1983.55.3.799.
5
Platelet-activating factor raises airway and vascular pressures and induces edema in lungs perfused with platelet-free solution.血小板活化因子可升高气道和血管压力，并在灌注无血小板溶液的肺中诱发水肿。
Am Rev Respir Dis. 1984 May;129(5):742-6. doi: 10.1164/arrd.1984.129.5.742.
6
Pressure effects and uptake of platelet-activating factor in isolated rat lung.压力对离体大鼠肺中血小板活化因子摄取的影响
J Appl Physiol Respir Environ Exerc Physiol. 1984 Oct;57(4):1039-44. doi: 10.1152/jappl.1984.57.4.1039.
7
Role of histamine in hypoxic pulmonary hypertension in the rat. I. Blockade or potentiation of endogenous amines, kinins, and ATP.组胺在大鼠低氧性肺动脉高压中的作用。I. 内源性胺类、激肽和三磷酸腺苷的阻断或增强作用
Circ Res. 1968 Mar;22(3):371-83. doi: 10.1161/01.res.22.3.371.
8
Is platelet activating factor (PAF) a mediator of endotoxin shock?血小板活化因子（PAF）是内毒素休克的介质吗？
Eur J Pharmacol. 1985 Feb 26;109(2):257-61. doi: 10.1016/0014-2999(85)90427-3.
9
Platelet activating factor (PAF) involvement in endotoxin-induced hypotension in rats. Studies with PAF-receptor antagonist kadsurenone.血小板活化因子（PAF）参与大鼠内毒素诱导的低血压。PAF受体拮抗剂海风藤酮的研究。
Biochem Biophys Res Commun. 1985 Mar 29;127(3):799-808. doi: 10.1016/s0006-291x(85)80014-0.
10
Effects of inhaled platelet activating factor on pulmonary function and bronchial responsiveness in man.吸入血小板活化因子对人体肺功能和支气管反应性的影响。
Lancet. 1986 Jul 26;2(8500):189-92. doi: 10.1016/s0140-6736(86)92489-x.

新型特异性血小板活化因子（PAF）拮抗剂WEB 2086可完全阻断PAF对大鼠离体肺支气管和血管的作用。

Bronchial and vascular effects of Paf in the rat isolated lung are completely blocked by WEB 2086, a novel specific Paf antagonist.

作者信息

Casals-Stenzel J, Franke J, Friedrich T, Lichey J

机构信息

Boehringer Ingelheim KG, Ingelheim, F.R.G.

出版信息

Br J Pharmacol. 1987 Aug;91(4):799-802. doi: 10.1111/j.1476-5381.1987.tb11278.x.

DOI:10.1111/j.1476-5381.1987.tb11278.x
PMID:3664079
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1853578/
Abstract

1 The effect of the platelet-activating factor (Paf) antagonist, WEB 2086, on Paf-induced increase of pulmonary artery perfusion pressure (Pp), bronchial inflation pressure (Pi) and wet-to-dry lung weight ratios (W/D) was investigated in the rat isolated lung. 2 Lungs were perfused with Krebs-Ringer solution (KRS) as controls or with KRS containing WEB 2086 (0.1, 1.0, 10.0 or 100 micrograms ml-1) and then injected with a bolus of 20 micrograms Paf. 3 A dose-related inhibition of the Paf-induced increase of Pp, Pi and W/D was observed, being almost maximal for the 10.0 micrograms ml-1 and complete for the 100 micrograms ml-1 doses of WEB 2086 when compared to controls. 4 It is concluded that WEB 2086 is a highly effective and specific Paf antagonist in the pulmonary vasculature and bronchial tract.

摘要

1 在大鼠离体肺中研究了血小板活化因子（Paf）拮抗剂WEB 2086对Paf诱导的肺动脉灌注压（Pp）、支气管充气压力（Pi）和肺湿重与干重比（W/D）升高的影响。2 用 Krebs-Ringer 溶液（KRS）灌注肺作为对照，或用含 WEB 2086（0.1、1.0、10.0 或 100 微克/毫升）的 KRS 灌注，然后注射 20 微克 Paf 推注剂量。3 观察到对 Paf 诱导的 Pp、Pi 和 W/D 升高有剂量相关的抑制作用，与对照相比，对于 10.0 微克/毫升的 WEB 2086 剂量，抑制作用几乎达到最大，对于 100 微克/毫升的剂量，抑制作用完全。4 结论是，WEB 2086 在肺血管系统和支气管中是一种高效且特异性的 Paf 拮抗剂。