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[F1865、马来酸氯苯那敏、地奈德和色甘酸钠经皮肤给药后的比较抗过敏和抗炎作用]

[Comparative antiallergic and anti-inflammatory action of F1865, mepyramine maleate, desonide and disodium cromoglycate after cutaneous administration].

作者信息

Tarayre J P, Aliaga M, Villanova G, Barbara M, Bru M, Caillol V, Lauressergues H

出版信息

J Pharmacol. 1984 Jan-Mar;15(1):37-51.

PMID:6425568
Abstract

The actions of F 1865 (ethyl 4' methoxy 4 phenyl thiazolyl 2 oxamate), an inhibitor of the release of histamine from mast cell, desonide, a corticosteroid, mepyramine maleate, an anti-H1 antihistaminic, and disodium cromoglycate were compared after cutaneous application in various experimental models of allergy and inflammation. F 1865 decreased IgE- and IgG-dependent passive cutaneous anaphylaxis in rats at doses having no effect on histamine- and serotonin-induced capillary permeability. Disodium cromoglycate showed the same activity spectrum, but its action was only found after intradermal application. The reduction of cutaneous anaphylaxis by desonide was found parallel to its inhibition of histamine effects, and to a lesser extent of serotonin effects. In the case of mepyramine, the antiallergic effect may be explained by its antihistaminic action. Desonide was highly active on cantharidin-induced non-immune inflammation and on non-immune and delayed hypersensitivity reactions induced by picryl chloride in mouse ear. Although far less active than the corticosteroid, F 1865, mepyramine and disodium cromoglycate did reduce the three types of reactions in mice. This evidenced a part played by histamine in such inflammations. Then it is likely that the inhibition of histamine release by F 1865 plays an important part in the effect of the compound observed in the various inflammations studied. However we cannot exclude actions against other mediators involved in these reactions.

摘要

在各种过敏和炎症实验模型中,对皮肤应用后肥大细胞组胺释放抑制剂F 1865(4'-甲氧基-4-苯基噻唑-2-草氨酸乙酯)、皮质类固醇地奈德、抗H1抗组胺药马来酸氯苯那敏和色甘酸钠的作用进行了比较。F 1865在对组胺和5-羟色胺诱导的毛细血管通透性无影响的剂量下,可降低大鼠中IgE和IgG依赖性被动皮肤过敏反应。色甘酸钠显示出相同的活性谱,但仅在皮内应用后才发现其作用。地奈德对皮肤过敏反应的减轻与其对组胺作用的抑制平行,对5-羟色胺作用的抑制程度较小。就马来酸氯苯那敏而言,其抗过敏作用可由其抗组胺作用来解释。地奈德对斑蝥素诱导的非免疫性炎症以及对小鼠耳部由苦味酸诱导的非免疫性和迟发性超敏反应具有高度活性。尽管F 1865、马来酸氯苯那敏和色甘酸钠的活性远低于皮质类固醇,但它们确实减轻了小鼠的这三种反应类型。这证明了组胺在这类炎症中起作用。那么,F 1865对组胺释放的抑制很可能在该化合物在所研究的各种炎症中观察到的效应中起重要作用。然而,我们不能排除其对这些反应中涉及的其他介质的作用。

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