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新型抗哮喘药物溴化氟托品对肥大细胞介质释放及介质作用的影响

[Effects of flutropium bromide, a new antiasthma drug, on mediator release from mast cells and actions of mediators].

作者信息

Misawa M, Yanaura S, Hosokawa T, Mizuno H, Irinoda K, Takahashi Y, Yoshimura K, Maruyama Y, Sugimoto K, Ohno H

机构信息

Department of Applied Pharmacology and Pharmacology, School of Pharmacy, Hoshi University, Tokyo, Japan.

出版信息

Nihon Yakurigaku Zasshi. 1988 Feb;91(2):97-103. doi: 10.1254/fpj.91.97.

Abstract

The effects of flutropium bromide (Ba598Br), a new antiasthma drug possessing the quarternary ammonium structure of atropine derivatives, on mediator release from mast cells and on actions of leukotriene (LT) D4 and serotonin were investigated. Flutropium bromide (3 and 10 mg/kg, i.v.) showed an inhibitory action on the 48 hr homologous PCA in guinea pigs. Atropine showed no inhibitory effect. Flutropium bromide also inhibited the release of histamine from isolated rat mast cells stimulated by antigen, although the inhibitory action was weaker than that of disodium cromoglycate. Atropine also had no inhibitory action in this case. Flutropium bromide and atropine showed no antagonistic action against LTD4-induced contraction of isolated tracheal smooth muscle of guinea pigs. Inhalation of flutropium bromide (0.3%) also showed no antagonistic action against serotonin-induced bronchoconstriction in dogs. From the above results, it is indicated that flutropium bromide has a weak mast cell stabilizing action, but no antagonistic action against LTD4 and serotonin.

摘要

研究了一种具有阿托品衍生物季铵结构的新型抗哮喘药物溴化氟托品(Ba598Br)对肥大细胞介质释放以及白三烯(LT)D4和5-羟色胺作用的影响。溴化氟托品(3和10毫克/千克,静脉注射)对豚鼠48小时同源被动皮肤过敏反应(PCA)具有抑制作用。阿托品无抑制作用。溴化氟托品还能抑制抗原刺激的离体大鼠肥大细胞释放组胺,尽管其抑制作用比色甘酸钠弱。在这种情况下,阿托品也无抑制作用。溴化氟托品和阿托品对豚鼠离体气管平滑肌由LTD4诱导的收缩无拮抗作用。吸入溴化氟托品(0.3%)对犬5-羟色胺诱导的支气管收缩也无拮抗作用。从上述结果表明,溴化氟托品具有较弱的肥大细胞稳定作用,但对LTD4和5-羟色胺无拮抗作用。

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