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组胺释放剂诱导的细胞内钙释放及其被某些抗过敏药物的抑制作用。

Intracellular calcium release induced by histamine releasers and its inhibition by some antiallergic drugs.

作者信息

Tasaka K, Mio M, Okamoto M

出版信息

Ann Allergy. 1986 Jun;56(6):464-9.

PMID:2424349
Abstract

When rat mast cells loaded with fluorescent Ca2+ indicator Quin 2 were exposed to either compound 48/80 (0.1 micrograms/mL) or substance P (2 microM) at 37 degrees C for 30 seconds in a Ca-free medium, a marked increase of Quin 2 fluorescence was noticed, indicating that Ca2+ was released from the intracellular Ca store. The pixel values of the whole cell image were displayed in a three dimensional projection. When mast cells were exposed to 48/80, the fluorescent increase was reflected as an increase of height and spreading of the image. When 0.01 to 1 mM of db-cAMP was pretreated for five minutes, an increase of Quin 2 fluorescence was inhibited in a dose-dependent fashion. Theophylline pretreatment also showed a preventive effect at 1 to 5 mM. A marked inhibition of the Quin 2 signal was induced by pretreatment with 0.01 mM of terfenadine (63.4% inhibition) or ketotifen (26.6% inhibition). Disodium cromoglycate also showed a similar inhibitory effect. In the measurement of the order parameters of liposomes, the addition of either terfenadine or ketotifen into the lipids increased the parameter value, indicating they provide the membrane stabilizing action.

摘要

当用荧光钙指示剂喹啉-2负载的大鼠肥大细胞在无钙培养基中于37℃下暴露于化合物48/80(0.1微克/毫升)或P物质(2微摩尔)30秒时,观察到喹啉-2荧光显著增加,表明钙离子从细胞内钙储存中释放出来。全细胞图像的像素值以三维投影显示。当肥大细胞暴露于48/80时,荧光增加表现为图像高度增加和扩散。当用0.01至1毫摩尔的二丁酰环磷腺苷(db-cAMP)预处理5分钟时,喹啉-2荧光的增加呈剂量依赖性受到抑制。茶碱预处理在1至5毫摩尔时也显示出预防作用。用0.01毫摩尔的特非那定(抑制率63.4%)或酮替芬(抑制率26.6%)预处理可诱导喹啉-2信号的显著抑制。色甘酸钠二钠也显示出类似的抑制作用。在脂质体序参数的测量中,向脂质中加入特非那定或酮替芬会增加参数值,表明它们具有膜稳定作用。

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