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某些黄嘌呤衍生物对气管平滑肌和骨骼肌的作用之间的解离。

Dissociation between the effects of some xanthine derivatives on the tracheal smooth muscle and on the skeletal muscle.

作者信息

Jeppsson A B, Johansson U, Waldeck B

出版信息

Acta Pharmacol Toxicol (Copenh). 1982 Aug;51(2):115-21. doi: 10.1111/j.1600-0773.1982.tb01000.x.

Abstract

The ability of some xanthine derivatives to relax the trachea, contracted by pilocarpine, and to increase the force of contraction of directly stimulated skeletal muscles from the guinea-pig was studied in vitro. No relationship was found between these two effects. Relaxation of the trachea occurred at lower concentrations and with a different order of potency as compared with the effects on the slow-contracting soleus muscle or on the fast-contracting extensor digitorum longus. One of the compounds, IBMX, 1-methyl-3-isobutyl-xanthine, showed an isoprenaline-like effect on the soleus muscle i.e. it depressed the force and fusion of subtetanic contractions. The relaxing effect of theophylline and IBMX on the trachea was additive to that of terbutaline but no clear potentiation was observed. The depression of the contraction of the soleus muscle elicited by terbutaline was reinforced by IBMX but not by theophylline. Theophylline in concentrations which used alone enhanced the contractions of the soleus muscle inhibited the effect of terbutaline. We conclude that the relative contribution of the various effects of xanthine derivatives differs from compound to compound.

摘要

在体外研究了某些黄嘌呤衍生物舒张由毛果芸香碱引起收缩的气管以及增强豚鼠直接刺激的骨骼肌收缩力的能力。未发现这两种效应之间存在关联。与对慢收缩的比目鱼肌或快收缩的趾长伸肌的效应相比,气管舒张发生在较低浓度且效价顺序不同。其中一种化合物,异丁基甲基黄嘌呤(IBMX),对比目鱼肌表现出类似异丙肾上腺素的效应,即它降低了不完全强直收缩的力量和融合。茶碱和IBMX对气管的舒张作用与特布他林的舒张作用相加,但未观察到明显的增强作用。IBMX增强了特布他林引起的比目鱼肌收缩抑制作用,而茶碱则无此作用。单独使用时能增强比目鱼肌收缩的茶碱浓度抑制了特布他林的作用。我们得出结论,黄嘌呤衍生物各种效应的相对贡献因化合物而异。

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