Characterization of platelet activating factor (PAF)-acether-induced contractions of guinea-pig lung strips by selected inhibitors of arachidonic acid metabolism and by PAF-acether antagonists

C TouvayP Braquet


The myotropic activities of PAF-acether, leukotriene B4, leukotriene D4 and histamine were compared on superfused guinea-pig lung parenchymal strip and were shown to have the following order of potency: PAF-acether greater than LTD4 greater than LTB4 greater than histamine. The contractile response of the lung parenchyma to PAF-acether was inhibited by aspirin, imidazole and OKY-046, which suggested that thromboxane A2 might play a mediator role in PAF-induced contractions. Neither an antagonist of leukotriene D4, FPL-55712, nor an antihistamine, mepyramine, had any effect on PAF contractions. The activity of a novel antagonist of PAF-acether, BN 52021, was also studied on superfused lung parenchyma contracted by histamine, leukotriene B4, leukotriene D4 and PAF-acether. This compound was without effect on the histamine response but it slightly reduced the contractions elicited by leukotriene D4 and potentiated those by leukotriene B4. BN 52021 (7.1 X 10(-6) M) inhibited by 63% the contraction induced by 5.7 X 10(-13) M PAF-acether and by 52% that induced by 5.7 X 10(-10) M PAF-acether and kadsurenone (8.4 X 10(-6) M), another PAF-acether antagonist, inhibited the same PAF-induced contractions by 75% and 20% respectively.


Jun 28, 1979·Nature·M ChignardJ Benveniste
Dec 1, 1980·Prostaglandins and Medicine·P SiroisG Girard
Jan 1, 1981·Annals of the New York Academy of Sciences·B B VargaftigF Wal
Oct 1, 1981·Journal of Medicinal Chemistry·K IizukaM Hayashi
Mar 16, 1981·Biochemical and Biophysical Research Communications·D J HanahanR N Pinckard


Related Concepts

FPL 55712
Imidazole sodium
Ozagrel, monohydrochloride, (E)-isomer
Kadsurenone, (2S-(2alpha,3beta,3abeta))-isomer
Ginkgolide B, (1beta)-isomer
Diterpenes, Labdane

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